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ty-2136b
- Development stage
- Phase 1
- Lead developer
- TYK Medicines
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
TY-2136b is an orally bioavailable, next-generation small molecule inhibitor that targets multiple receptor tyrosine kinases, specifically anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), and tropomyosin-related kinases (TRK; NTRK1/2/3). It is designed to overcome resistance mutations in these kinases, such as ROS1 G2032R and TRKA G595R, which are associated with acquired resistance to earlier therapies. TY-2136b has demonstrated potent inhibition of these targets in preclinical models and shows dose-dependent antitumor activity in xenograft models harboring relevant mutations. The drug is currently being evaluated in phase 1 clinical trials for patients with advanced or metastatic solid tumors harboring ALK, ROS1, or NTRK gene alterations[1][2][3][4][5][6]. The developer is TYK Medicines.
- Other names
- ty-2136ty2136ty 2136
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK3 (Tropomyosin receptor kinase C)NTRK1 (Tropomyosin-related receptor kinase A)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)LTK (Leukocyte receptor tyrosine kinase)
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