(Amendment No. 5)1
Check the appropriate box
to designate the rule pursuant to which this Schedule is filed:
The information required
on the remainder of this cover page shall not be deemed to be “filed” for the purpose of Section 18 of the Securities
Exchange Act of 1934 (“Act”) or otherwise subject to the liabilities of that section of the Act but shall be subject
to all other provisions of the Act (however, see the Notes).
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1
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NAME OF REPORTING PERSON
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Biotechnology Value Fund, L.P.
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2
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CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
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(a) ☒
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(b) ☐
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3
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SEC USE ONLY
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4
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CITIZENSHIP OR PLACE OF ORGANIZATION
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Delaware
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NUMBER OF
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5
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SOLE VOTING POWER
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SHARES
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BENEFICIALLY
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0 shares
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OWNED BY
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6
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SHARED VOTING POWER
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EACH
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REPORTING
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4,184,109 (1)
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PERSON WITH
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7
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SOLE DISPOSITIVE POWER
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0 shares
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8
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SHARED DISPOSITIVE POWER
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4,184,109 (1)
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9
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AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
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4,184,109 (1)
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10
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CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
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☐
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11
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PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
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6.0% (1)
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12
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TYPE OF REPORTING PERSON
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PN
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(1) Includes 1,285,424 shares of Common Stock
issuable upon the exercise of A-1 Warrants (defined in Item 4).
Includes 1,081,685 shares of Common Stock issuable
upon the exercise of A-2 Warrants (defined in Item 4). Excludes A-2 Warrants to acquire 2,045,025 shares of Common Stock as a result
of the A-2 Warrants Blocker (defined in Item 4).
Excludes A-3 Warrants (defined in Item 4) to
acquire 1,362,750 shares of Common Stock as a result of the A-3 Warrants Blocker (defined in Item 4).
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1
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NAME OF REPORTING PERSON
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BVF I GP LLC
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2
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CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
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(a) ☒
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(b) ☐
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3
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SEC USE ONLY
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4
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CITIZENSHIP OR PLACE OF ORGANIZATION
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Delaware
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NUMBER OF
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5
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SOLE VOTING POWER
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SHARES
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BENEFICIALLY
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0 shares
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OWNED BY
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6
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SHARED VOTING POWER
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EACH
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REPORTING
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4,184,109 (1)
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PERSON WITH
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7
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SOLE DISPOSITIVE POWER
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0 shares
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8
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SHARED DISPOSITIVE POWER
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4,184,109 (1)
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9
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AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
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4,184,109 (1)
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10
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CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
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☐
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11
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PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
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6.0% (1)
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12
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TYPE OF REPORTING PERSON
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OO
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(1) Includes 1,285,424 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Includes 1,081,685 shares of Common Stock issuable
upon the exercise of A-2 Warrants. Excludes A-2 Warrants to acquire 2,045,025 shares of Common Stock as a result of the A-2 Warrants
Blocker.
Excludes A-3 Warrants to acquire 1,362,750
shares of Common Stock as a result of the A-3 Warrants Blocker.
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1
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NAME OF REPORTING PERSON
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Biotechnology Value Fund II, L.P.
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2
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CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
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(a) ☒
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(b) ☐
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3
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SEC USE ONLY
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4
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CITIZENSHIP OR PLACE OF ORGANIZATION
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Delaware
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NUMBER OF
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5
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SOLE VOTING POWER
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SHARES
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BENEFICIALLY
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0 shares
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OWNED BY
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6
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SHARED VOTING POWER
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EACH
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REPORTING
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2,360,109 (1)
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PERSON WITH
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7
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SOLE DISPOSITIVE POWER
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0 shares
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8
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SHARED DISPOSITIVE POWER
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2,360,109 (1)
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9
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AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
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2,360,109 (1)
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10
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CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
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☐
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11
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PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
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3.5% (1)
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12
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TYPE OF REPORTING PERSON
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PN
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(1) Includes 1,083,457 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Excludes A-2 Warrants to acquire 2,635,450
shares of Common Stock as a result of the A-2 Warrants Blocker.
Excludes A-3 Warrants to acquire 957,489 shares
of Common Stock as a result of the A-3 Warrants Blocker.
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1
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NAME OF REPORTING PERSON
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BVF II GP LLC
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2
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CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
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(a) ☒
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(b) ☐
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3
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SEC USE ONLY
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4
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CITIZENSHIP OR PLACE OF ORGANIZATION
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Delaware
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NUMBER OF
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5
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SOLE VOTING POWER
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SHARES
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BENEFICIALLY
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0 shares
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OWNED BY
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6
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SHARED VOTING POWER
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EACH
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REPORTING
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2,360,109 (1)
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PERSON WITH
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7
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SOLE DISPOSITIVE POWER
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0 shares
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8
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SHARED DISPOSITIVE POWER
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2,360,109 (1)
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9
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AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
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2,360,109 (1)
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10
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CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
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☐
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11
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PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
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3.5% (1)
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12
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TYPE OF REPORTING PERSON
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OO
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(1) Includes 1,083,457 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Excludes A-2 Warrants to acquire 2,635,450
shares of Common Stock as a result of the A-2 Warrants Blocker.
Excludes A-3 Warrants to acquire 957,489 shares
of Common Stock as a result of the A-3 Warrants Blocker.
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1
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NAME OF REPORTING PERSON
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Biotechnology Value Trading Fund OS LP
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2
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CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
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(a) ☒
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(b) ☐
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3
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SEC USE ONLY
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4
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CITIZENSHIP OR PLACE OF ORGANIZATION
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Cayman Islands
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NUMBER OF
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5
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SOLE VOTING POWER
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SHARES
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BENEFICIALLY
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0 shares
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OWNED BY
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6
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SHARED VOTING POWER
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EACH
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REPORTING
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381,750 (1)
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PERSON WITH
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7
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SOLE DISPOSITIVE POWER
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0 shares
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8
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SHARED DISPOSITIVE POWER
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381,750 (1)
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9
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AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
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381,750 (1)
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10
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CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
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☐
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11
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PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
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Less than 1% (1)
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12
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TYPE OF REPORTING PERSON
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PN
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(1) Includes 178,494 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Excludes A-2 Warrants to acquire 434,190 shares
of Common Stock as a result of the A-2 Warrants Blocker.
Excludes A-3 Warrants to acquire 152,442 shares
of Common Stock as a result of the A-3 Warrants Blocker.
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1
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NAME OF REPORTING PERSON
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BVF Partners OS Ltd.
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2
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CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
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(a) ☒
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(b) ☐
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3
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SEC USE ONLY
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4
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CITIZENSHIP OR PLACE OF ORGANIZATION
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Cayman Islands
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NUMBER OF
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5
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SOLE VOTING POWER
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SHARES
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BENEFICIALLY
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0 shares
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OWNED BY
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6
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SHARED VOTING POWER
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EACH
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REPORTING
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381,750 (1)
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PERSON WITH
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7
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SOLE DISPOSITIVE POWER
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0 shares
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8
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SHARED DISPOSITIVE POWER
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381,750 (1)
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9
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AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
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381,750 (1)
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10
|
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CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
|
☐
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11
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PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
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|
|
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Less than 1% (1)
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12
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TYPE OF REPORTING PERSON
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|
CO
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(1) Includes 178,494 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Excludes A-2 Warrants to acquire 434,190 shares
of Common Stock as a result of the A-2 Warrants Blocker.
Excludes A-3 Warrants to acquire 152,442 shares
of Common Stock as a result of the A-3 Warrants Blocker.
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1
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NAME OF REPORTING PERSON
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BVF GP HOLDINGS LLC
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2
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CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
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(a) ☒
|
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(b) ☐
|
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3
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SEC USE ONLY
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4
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CITIZENSHIP OR PLACE OF ORGANIZATION
|
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|
|
|
|
|
|
|
|
|
Delaware
|
|
NUMBER OF
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5
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SOLE VOTING POWER
|
|
SHARES
|
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|
|
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|
BENEFICIALLY
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|
0 shares
|
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OWNED BY
|
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6
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SHARED VOTING POWER
|
|
EACH
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|
|
|
|
|
REPORTING
|
|
|
|
|
6,544,218 (1)
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PERSON WITH
|
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7
|
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SOLE DISPOSITIVE POWER
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|
|
|
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|
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0 shares
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|
|
8
|
|
SHARED DISPOSITIVE POWER
|
|
|
|
|
|
|
|
|
|
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|
6,544,218 (1)
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|
9
|
|
AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
6,544,218 (1)
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|
10
|
|
CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
|
☐
|
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|
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|
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|
11
|
|
PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
|
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|
|
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|
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9.3% (1)
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12
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TYPE OF REPORTING PERSON
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|
OO
|
|
(1) Includes 2,368,881 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Includes 1,081,685 shares of Common Stock issuable
upon the exercise of A-2 Warrants. Excludes A-2 Warrants to acquire 4,680,475 shares of Common Stock as a result of the A-2 Warrants
Blocker.
Excludes A-3 Warrants to acquire 2,320,239
shares of Common Stock as a result of the A-3 Warrants Blocker.
|
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1
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NAME OF REPORTING PERSON
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|
BVF Partners L.P.
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2
|
|
CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
|
(a) ☒
|
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(b) ☐
|
|
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|
3
|
|
SEC USE ONLY
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
4
|
|
CITIZENSHIP OR PLACE OF ORGANIZATION
|
|
|
|
|
|
|
|
|
|
|
Delaware
|
|
NUMBER OF
|
|
5
|
|
SOLE VOTING POWER
|
|
SHARES
|
|
|
|
|
|
BENEFICIALLY
|
|
|
|
|
0 shares
|
|
OWNED BY
|
|
6
|
|
SHARED VOTING POWER
|
|
EACH
|
|
|
|
|
|
REPORTING
|
|
|
|
|
7,050,464 (1)
|
|
PERSON WITH
|
|
7
|
|
SOLE DISPOSITIVE POWER
|
|
|
|
|
|
|
|
|
|
|
|
|
0 shares
|
|
|
|
8
|
|
SHARED DISPOSITIVE POWER
|
|
|
|
|
|
|
|
|
|
|
|
|
7,050,464 (1)
|
|
|
9
|
|
AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
7,050,464 (1)
|
|
|
10
|
|
CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
|
☐
|
|
|
|
|
|
|
|
|
|
|
|
|
11
|
|
PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
|
|
|
|
|
|
|
|
|
|
|
9.99% (1)
|
|
|
12
|
|
TYPE OF REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
PN, IA
|
|
(1) Includes 2,592,572 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Includes 1,081,685 shares of Common Stock issuable
upon the exercise of A-2 Warrants. Excludes A-2 Warrants to acquire 5,224,595 shares of Common Stock as a result of the A-2 Warrants
Blocker.
Excludes A-3 Warrants to acquire 2,532,155 shares of Common Stock
as a result of the A-3 Warrants Blocker.
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
1
|
|
NAME OF REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
BVF Inc.
|
|
|
2
|
|
CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
|
(a) ☒
|
|
|
|
|
(b) ☐
|
|
|
|
|
|
|
|
3
|
|
SEC USE ONLY
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
4
|
|
CITIZENSHIP OR PLACE OF ORGANIZATION
|
|
|
|
|
|
|
|
|
|
|
Delaware
|
|
NUMBER OF
|
|
5
|
|
SOLE VOTING POWER
|
|
SHARES
|
|
|
|
|
|
BENEFICIALLY
|
|
|
|
|
0 shares
|
|
OWNED BY
|
|
6
|
|
SHARED VOTING POWER
|
|
EACH
|
|
|
|
|
|
REPORTING
|
|
|
|
|
7,050,464 (1)
|
|
PERSON WITH
|
|
7
|
|
SOLE DISPOSITIVE POWER
|
|
|
|
|
|
|
|
|
|
|
|
|
0 shares
|
|
|
|
8
|
|
SHARED DISPOSITIVE POWER
|
|
|
|
|
|
|
|
|
|
|
|
|
7,050,464 (1)
|
|
|
9
|
|
AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
7,050,464 (1)
|
|
|
10
|
|
CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
|
☐
|
|
|
|
|
|
|
|
|
|
|
|
|
11
|
|
PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
|
|
|
|
|
|
|
|
|
|
|
9.99% (1)
|
|
|
12
|
|
TYPE OF REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
CO
|
|
(1) Includes 2,592,572 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Includes 1,081,685 shares of Common Stock issuable
upon the exercise of A-2 Warrants. Excludes A-2 Warrants to acquire 5,224,595 shares of Common Stock as a result of the A-2 Warrants
Blocker.
Excludes A-3 Warrants to acquire 2,532,155
shares of Common Stock as a result of the A-3 Warrants Blocker.
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
1
|
|
NAME OF REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
Mark N. Lampert
|
|
|
2
|
|
CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP
|
(a) ☒
|
|
|
|
|
(b) ☐
|
|
|
|
|
|
|
|
3
|
|
SEC USE ONLY
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
4
|
|
CITIZENSHIP OR PLACE OF ORGANIZATION
|
|
|
|
|
|
|
|
|
|
|
United States
|
|
NUMBER OF
|
|
5
|
|
SOLE VOTING POWER
|
|
SHARES
|
|
|
|
|
|
BENEFICIALLY
|
|
|
|
|
0 shares
|
|
OWNED BY
|
|
6
|
|
SHARED VOTING POWER
|
|
EACH
|
|
|
|
|
|
REPORTING
|
|
|
|
|
7,050,464 (1)
|
|
PERSON WITH
|
|
7
|
|
SOLE DISPOSITIVE POWER
|
|
|
|
|
|
|
|
|
|
|
|
|
0 shares
|
|
|
|
8
|
|
SHARED DISPOSITIVE POWER
|
|
|
|
|
|
|
|
|
|
|
|
|
7,050,464 (1)
|
|
|
9
|
|
AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
7,050,464 (1)
|
|
|
10
|
|
CHECK BOX IF THE
AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES
|
☐
|
|
|
|
|
|
|
|
|
|
|
|
|
11
|
|
PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)
|
|
|
|
|
|
|
|
|
|
|
9.99% (1)
|
|
|
12
|
|
TYPE OF REPORTING PERSON
|
|
|
|
|
|
|
|
|
|
|
IN
|
|
(1) Includes 2,592,572 shares of Common Stock
issuable upon the exercise of A-1 Warrants.
Includes 1,081,685 shares of Common Stock issuable
upon the exercise of A-2 Warrants. Excludes A-2 Warrants to acquire 5,224,595 shares of Common Stock as a result of the A-2 Warrants
Blocker.
Excludes A-3 Warrants to acquire 2,532,155 shares of Common Stock
as a result of the A-3 Warrants Blocker.
|
Item 1(a).
|
Name of Issuer:
|
Regulus Therapeutics Inc., a Delaware corporation (the “Issuer”).
|
Item 1(b).
|
Address of Issuer’s Principal Executive Offices:
|
10628 Science Center Drive, Suite 225
San Diego, California 92121
|
Item 2(a).
|
Name of Person Filing
|
|
Item 2(b).
|
Address of Principal Business Office or, if None, Residence
|
Biotechnology Value Fund, L.P. (“BVF”)
44 Montgomery St., 40th Floor
San Francisco, California 94104
Citizenship: Delaware
BVF I GP LLC (“BVF GP”)
44 Montgomery St., 40th Floor
San Francisco, California 94104
Citizenship: Delaware
Biotechnology Value Fund II, L.P. (“BVF2”)
44 Montgomery St., 40th Floor
San Francisco, California 94104
Citizenship: Delaware
BVF II GP LLC (“BVF2 GP”)
44 Montgomery St., 40th Floor
San Francisco, California 94104
Citizenship: Delaware
Biotechnology Value Trading Fund OS
LP (“Trading Fund OS”)
PO Box 309 Ugland House
Grand Cayman, KY1-1104
Cayman Islands
Citizenship: Cayman Islands
BVF Partners OS Ltd. (“Partners
OS”)
PO Box 309 Ugland House
Grand Cayman, KY1-1104
Cayman Islands
Citizenship: Cayman Islands
BVF GP Holdings LLC (“BVF GPH”)
44 Montgomery St., 40th Floor
San Francisco, California 94104
Citizenship: Delaware
BVF Partners L.P. (“Partners”)
44 Montgomery St., 40th Floor
San Francisco, California 94104
Citizenship: Delaware
BVF Inc.
44 Montgomery St., 40th Floor
San Francisco, California 94104
Citizenship: Delaware
Mark N. Lampert (“Mr. Lampert”)
44 Montgomery St., 40th Floor
San Francisco, California 94104
Citizenship: United States
Each of the foregoing is referred to
as a “Reporting Person” and collectively as the “Reporting Persons.”
|
Item 2(d).
|
Title of Class of Securities:
|
Common Stock, par value $0.001 per
share (the “Common Stock”)
75915K200
|
Item 3.
|
If This Statement is Filed Pursuant to Rule 13d-1(b), or 13d-2(b) or (c), Check Whether the Person
Filing is a:
|
|
|
/x/
|
Not applicable.
|
|
|
|
|
|
(a)
|
/ /
|
Broker or dealer registered under Section 15 of the Exchange Act.
|
|
|
|
|
|
(b)
|
/ /
|
Bank as defined in Section 3(a)(6) of the Exchange Act.
|
|
|
|
|
|
(c)
|
/ /
|
Insurance company as defined in Section 3(a)(19) of the Exchange Act.
|
|
|
|
|
|
(d)
|
/ /
|
Investment company registered under Section 8 of the Investment Company Act.
|
|
|
|
|
|
(e)
|
/ /
|
An investment adviser in accordance with Rule 13d-1(b)(1)(ii)(E).
|
|
|
|
|
|
(f)
|
/ /
|
An employee benefit plan or endowment fund in accordance with Rule 13d-1(b)(1)(ii)(F).
|
|
|
|
|
|
(g)
|
/ /
|
A parent holding company or control person in accordance with Rule 13d-1(b)(1)(ii)(G).
|
|
|
|
|
|
(h)
|
/ /
|
A savings association as defined in Section 3(b) of the Federal Deposit Insurance Act.
|
|
|
|
|
|
(i)
|
/ /
|
A church plan that is excluded from the definition of an investment company under Section 3(c)(14) of the Investment Company Act.
|
|
|
|
|
|
(j)
|
/ /
|
Group, in accordance with Rule 13d-1(b)(1)(ii)(J).
|
|
|
|
|
|
(k)
|
/ /
|
Group, in accordance with Rule 240.13d-1(b)(1)(ii)(K). If filing as a non-U.S. institution in accordance with Rule 240.13d-1(b)(1)(ii)(J), please specify the type of institution: ____
|
|
(a)
|
Amount beneficially owned:
|
The Reporting Persons hold 2,592,572
A-1 Warrants (the “A-1 Warrants”) exercisable for an aggregate of 2,592,572 shares of Common Stock. The A-1 Warrants
are exercisable for a period of five years following the date of issuance and have an exercise price of $1.08 per share. The A-1
Warrants may not be exercised if, after such exercise, the Reporting Persons would beneficially own, as determined in accordance
with Section 13(d) of the Securities Exchange Act of 1934, as amended (the “Exchange Act”), more than 9.99% of the
number of shares of Common Stock then issued and outstanding (the “A-1 Warrants Blocker”). As of the close of business
on December 31, 2020, the A-1 Warrants Blocker limits the aggregate exercise of A-1 Warrants by the Reporting Persons to 2,592,572
out of the 2,592,572 shares of Common Stock underlying the A-1 Warrants owned by the Reporting Persons in the aggregate. In providing
beneficial ownership described herein, the Reporting Persons have assumed that all A-1 Warrants owned by each of BVF, BVF2 and
Trading Fund OS and held in a certain Partners managed account (the “Partners Managed Account”) would be exercised.
The Reporting Persons hold 6,306,280
A-2 Warrants (the “A-2 Warrants”) exercisable for an aggregate of 6,306,280 shares of Common Stock. The A-2 Warrants
are exercisable for a period of five years following the date of issuance and have an exercise price of $6.66 per share. The A-2
Warrants may not be exercised if, after such exercise, the Reporting Persons would beneficially own, as determined in accordance
with Section 13(d) of the Exchange Act, more than 9.99% of the number of shares of Common Stock then issued and outstanding (the
“A-2 Warrants Blocker”). As of the close of business on December 31, 2020, the A-2 Warrants Blocker limits the aggregate
exercise of A-2 Warrants by the Reporting Persons to 1,081,685 out of the 6,306,280 shares of Common Stock underlying the A-2 Warrants
owned by the Reporting Persons in the aggregate. In providing beneficial ownership described herein, the Reporting Persons have
assumed that A-2 Warrants held by BVF to acquire 1,081,685 shares of Common Stock would be exercised, which would bring the Reporting
Persons to the aggregate 9.99% limitation, and the remaining A-2 Warrants exercisable into 2,045,025 shares of Common Stock owned
by BVF, A-2 Warrants exercisable into 2,635,450 shares of Common Stock owned by BVF2, A-2 Warrants exercisable into 434,190 shares
of Common Stock owned by Trading Fund OS, and the A-2 Warrants exercisable into 109,930 shares of Common Stock held in the Partners
Managed Account, would not be exercised due to the A-2 Warrants Blocker.
The Reporting Persons hold 2,532,155
A-3 Warrants (the “A-3 Warrants”) exercisable for an aggregate of 2,532,155 shares of Common Stock. The A-3 Warrants
are exercisable for a period of five years following the date of issuance and have an exercise price of $0.7464 per share. The
A-3 Warrants may not be exercised if, after such exercise, the Reporting Persons would beneficially own, as determined in accordance
with Section 13(d) of the Exchange Act, more than 9.99% of the number of shares of Common Stock then issued and outstanding (the
“A-3 Warrants Blocker”). As of the close of business on December 31, 2020, the A-3 Warrants Blocker limits the aggregate
exercise of A-3 Warrants by the Reporting Persons to 0 out of the 2,532,155 shares of Common Stock underlying the A-3 Warrants
owned by the Reporting Persons in the aggregate. In providing beneficial ownership described herein, the Reporting Persons have
assumed the A-3 Warrants owned by each of BVF, BVF2 and Trading Fund OS and held in the Partners Managed Account would not be exercised
due to the A-3 Warrants Blocker.
As of the close of business on December
31, 2020, (i) BVF beneficially owned 4,184,109 shares of Common Stock, including 1,285,424 shares of Common Stock issuable upon
the exercise of the A-1 Warrants held by it and 1,081,685 shares of Common Stock issuable upon the exercise of the A-2 Warrants
held by it, and excluding (a) 2,045,025 shares of Common Stock issuable upon the exercise of A-2 Warrants held by it, and (b) 1,362,750
shares of Common Stock issuable upon the exercise of A-3 Warrants held by it; (ii) BVF2 beneficially owned 2,360,109 shares of
Common Stock, including 1,083,457 shares of Common Stock issuable upon the exercise of the A-1 Warrants held by it, and excluding
(a) 2,635,450 shares of Common Stock issuable upon the exercise of A-2 Warrants held by it, and (b) 957,489 shares of Common Stock
issuable upon the exercise of A-3 Warrants held by it; and (iii) Trading Fund OS beneficially owned 381,750 shares of Common Stock,
including 178,494 shares of Common Stock issuable upon the exercise of the A-1 Warrants held by it, and excluding (a) 434,190 shares
of Common Stock issuable upon the exercise of A-2 Warrants held by it, and (b) 152,442 shares of Common Stock issuable upon the
exercise of A-3 Warrants held by it.
BVF GP, as the general partner of BVF,
may be deemed to beneficially own the 4,184,109 shares of Common Stock beneficially owned by BVF.
BVF2 GP, as the general partner of
BVF2, may be deemed to beneficially own the 2,360,109 shares of Common Stock beneficially owned by BVF2.
Partners OS, as the general partner
of Trading Fund OS, may be deemed to beneficially own the 381,750 shares of Common Stock beneficially owned by Trading Fund OS.
BVF GPH, as the sole member of each
of BVF GP and BVF2 GP, may be deemed to beneficially own the 6,544,218 shares of Common Stock beneficially owned in the aggregate
by BVF and BVF2.
Partners, as the investment manager
of BVF, BVF2 and Trading Fund OS, and the sole member of Partners OS, may be deemed to beneficially own the 7,050,464 Shares beneficially
owned in the aggregate by BVF, BVF2, Trading Fund OS, and the Partners Managed Account, including 124,496 shares of Common Stock
held in the Partners Managed Account, which includes 45,197 shares of Common Stock issuable upon the exercise of A-1 Warrants held
in the Partners Managed Account, and excluding (a) 109,930 shares of Common Stock issuable upon the exercise of A-2 Warrants held
in the Partners Managed Account, and (b) 59,474 shares of Common Stock issuable upon the exercise of A-3 Warrants held in the Partners
Managed Account.
BVF Inc., as the general partner of
Partners, may be deemed to beneficially own the 7,050,464 shares of Common Stock beneficially owned by Partners.
Mr. Lampert, as a director and officer
of BVF Inc., may be deemed to beneficially own the 7,050,464 shares of Common Stock beneficially owned by BVF Inc.
The foregoing should not be construed
in and of itself as an admission by any Reporting Person as to beneficial ownership of any shares of Common Stock owned by another
Reporting Person. BVF GP disclaims beneficial ownership of the shares of Common Stock beneficially owned by BVF. BVF2 GP disclaims
beneficial ownership of the shares of Common Stock beneficially owned by BVF2. Partners OS disclaims beneficial ownership of the
shares of Common Stock beneficially owned by Trading Fund OS. BVF GPH disclaims beneficial ownership of the shares of Common Stock
beneficially owned by BVF and BVF2. Each of Partners, BVF Inc. and Mr. Lampert disclaims beneficial ownership of the shares of
Common Stock beneficially owned by BVF, BVF2, Trading Fund OS, and held in the Partners Managed Account, and the filing of this
statement shall not be construed as an admission that any such person or entity is the beneficial owner of any such securities.
The following percentages are based on a denominator that is the sum of (i) 66,900,962 shares of Common Stock outstanding as of December
11, 2020 as set forth in the Issuer’s Registration Statement on Form S-3 filed with the Securities and Exchange Commission on December
31, 2020 and (ii) certain or all of the 2,592,572 shares of Common Stock issuable upon the exercise of A-1 Warrants and 1,081,685 shares
of Common Stock issuable upon the exercise of A-2 Warrants, as applicable.
As of the close of business on December
31, 2020, (i) BVF beneficially owned approximately 6.0% of the outstanding shares of Common Stock, (ii) BVF2 beneficially owned
approximately 3.5% of the outstanding shares of Common Stock, (iii) Trading Fund OS beneficially owned less than 1% of the outstanding
shares of Common Stock, (iv) BVF GP may be deemed to beneficially own approximately 6.0% of the outstanding shares of Common Stock,
(v) BVF2 GP may be deemed to beneficially own approximately 3.5% of the outstanding shares of Common Stock, (vi) Partners OS may
be deemed to beneficially own less than 1% of the outstanding shares of Common Stock, (vii) BVF GPH may be deemed to beneficially
own approximately 9.3% of the outstanding shares of Common Stock, and (viii) each of Partners, BVF Inc. and Mr. Lampert may be
deemed to beneficially own approximately 9.99% of the outstanding shares of Common Stock (less than 1% of the outstanding shares
of Common Stock are held in the Partners Managed Account).
|
(c)
|
Number of shares as to which such person has:
|
|
(i)
|
Sole power to vote or to direct the vote
|
See Cover Pages Items 5-9.
|
(ii)
|
Shared power to vote or to direct the vote
|
See Cover Pages Items 5-9.
|
(iii)
|
Sole power to dispose or to direct the disposition of
|
See Cover Pages Items 5-9.
|
(iv)
|
Shared power to dispose or to direct the disposition of
|
See Cover Pages Items 5-9.
|
Item 5.
|
Ownership of Five Percent or Less of a Class.
|
Not Applicable.
|
Item 6.
|
Ownership of More than Five Percent on Behalf of Another Person.
|
BVF GP, BVF GPH, Partners, BVF Inc.
and Mr. Lampert share voting and dispositive power over the shares of Common Stock beneficially owned by BVF. BVF GPH, Partners,
BVF Inc. and Mr. Lampert share voting and dispositive power over the shares of Common Stock beneficially owned by BVF2. Partners,
BVF Inc. and Mr. Lampert share voting and dispositive power over the shares of Common Stock beneficially owned by Trading Fund
OS and the Partners Managed Account.
|
Item 7.
|
Identification and Classification of the Subsidiary That Acquired the Security Being Reported on
by the Parent Holding Company or Control Person.
|
Not Applicable.
|
Item 8.
|
Identification and Classification of Members of the Group.
|
See Exhibit 99.1 to Amendment No. 4
to the Schedule 13G filed with the Securities and Exchange Commission on February 14, 2020.
|
Item 9.
|
Notice of Dissolution of Group.
|
Not Applicable.
By signing below each of
the undersigned certifies that, to the best of its knowledge and belief, the securities referred to above were not acquired and
are not held for the purpose of or with the effect of changing or influencing the control of the issuer of the securities and were
not acquired and are not held in connection with or as a participant in any transaction having that purpose or effect.
SIGNATURE
After reasonable inquiry
and to the best of his knowledge and belief, each of the undersigned certifies that the information set forth in this statement
is true, complete and correct.
Dated: February 12, 2021
BIOTECHNOLOGY VALUE FUND, L.P.
|
|
BIOTECHNOLOGY VALUE TRADING FUND OS LP
|
|
|
|
|
By:
|
BVF I GP LLC., its general partner
|
|
By:
|
BVF Partners L.P., its investment manager
|
|
|
|
By:
|
BVF Inc., its general partner
|
By:
|
/s/ Mark N. Lampert
|
|
|
|
|
Mark N. Lampert
|
|
By:
|
/s/ Mark N. Lampert
|
|
Chief Executive Officer
|
|
|
Mark N. Lampert
|
|
|
|
|
President
|
|
|
|
|
|
BVF I GP LLC
|
|
|
|
|
|
|
BVF GP HOLDINGS LLC
|
By:
|
/s/ Mark N. Lampert
|
|
|
|
Mark N. Lampert
|
|
By:
|
/s/ Mark N. Lampert
|
|
Chief Executive Officer
|
|
|
Mark N. Lampert
|
|
|
|
|
Chief Executive Officer
|
|
|
|
|
|
BIOTECHNOLOGY VALUE FUND II, L.P.
|
|
|
|
|
|
BVF PARTNERS L.P.
|
By:
|
BVF II GP LLC, its general partner
|
|
|
|
|
|
By:
|
BVF Inc., its general partner
|
By:
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/s/ Mark N. Lampert
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Mark N. Lampert
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By:
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/s/ Mark N. Lampert
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Chief Executive Officer
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Mark N. Lampert
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President
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BVF II GP LLC
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BVF INC.
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By:
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/s/ Mark N. Lampert
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Mark N. Lampert
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By:
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/s/ Mark N. Lampert
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Chief Executive Officer
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Mark N. Lampert
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President
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BVF PARTNERS OS LTD.
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/s/ Mark N. Lampert
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By:
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BVF Partners L.P., its sole member
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MARK N. LAMPERT
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By:
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BVF Inc., its general partner
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By:
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/s/ Mark N. Lampert
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Mark N. Lampert
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President
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