SHANGHAI, May 24, 2024
/PRNewswire/ -- Tyligand Bioscience, a clinical-stage
biotechnology company focused on the discovery and development of
innovative cancer therapies, announced that the first patient had
been dosed in the Phase 1/2 trial of TSN1611 for the treatment of
KRAS G12D mutant solid tumors in the
United States. The program has been cleared for IND by U.S.
FDA and China NMPA in Feb and April
2024, respectively.
TSN1611 is a highly selective and orally bioavailable small
molecule targeting the G12D mutant of KRAS oncogene, with excellent
enzymatic and cellular activities. It effectively engages both the
ON-state (GTP-bound) and OFF-state (GDP-bound) of KRAS G12D.
TSN1611 has demonstrated superior in vivo anti-tumor
activity with a durable response across multiple animal models.
TSN1611 features favorable physicochemical properties, oral
pharmacokinetic profiles, and notable brain penetration potential
to address a large unmet medical need.
The ongoing first-in-human, multi-center clinical trial
(NCT06385925) is designed to assess the safety, tolerability,
pharmacokinetic profile, and preliminary anti-tumor activity in
patients with advanced solid tumors harboring the KRAS G12D
mutation. Patient recruitment is currently underway in the United States, with plans to initiate in
China in the coming months.
"Preclinical profile indicated the potential of TSN1611 as a
best-in-class molecule for treating cancers driven by KRAS
G12D," said Dr.
Tony Zhang, PhD., CEO of Tyligand
Bioscience, "We are proud of our teams for the creativity,
quality and speed in the discovery and early development efforts,
and grateful for the support from our partners and investors in
advancing TSN1611 one step closer toward the patients in
need."
About Tyligand Bioscience:
Founded in 2018, Tyligand Bioscience is a clinical stage biotech
focusing on the discovery and development of transformative
therapies for cancer. In addition to the KRAS G12D program, the
company has several molecules in development, including TSN084, a
Type II multi-kinase inhibitor; TSN222, a first in kind dual acting
tumor immune agonist (DATIA®), and a platform for
antibody drug conjugates (ADCs) featuring proprietary linkers and
novel payloads. For more information about Tyligand
Bioscience, please visit www.tyligand.com.
KRAS mutations
are the most common driver oncogenes, implicated in approximately
25% of all human cancers, with KRAS G12D emerging as a predominant
isoform, which is particularly prevalent in pancreatic, colorectal,
and non-small cell lung cancers. There exists an urgent need for
effective therapies targeting KRAS G12D to improve patient
outcomes.
CONTACT: Tyligand Bioscience, info@tyligand.com,
https://www.tyligand.com
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SOURCE Tyligand Bioscience