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Drug intelligence / Profile preview
relcobatinib
- Development stage
- Phase 3
- Lead developer
- Enliven Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Relcobatinib (ELVN-001) is an investigational, potent, highly selective, and ATP-competitive small molecule kinase inhibitor designed to target the BCR::ABL1 gene fusion, which is the oncogenic driver of chronic myeloid leukemia (CML). Developed by Enliven Therapeutics, relcobatinib binds to a unique P-loop 'folded-in' active conformation of the ABL1 kinase domain, creating a narrow selectivity tunnel that avoids off-target activity against other kinases such as PDGFR, KIT, VEGFR2, and the Src family. It is designed to overcome resistance mutations, including the gatekeeper T315I mutation and myristoyl pocket mutations (e.g., A334P, P465S) that confer resistance to allosteric inhibitors like asciminib. Relcobatinib is currently in clinical development, with a pivotal Phase 3 trial (ENABLE-2) evaluating its efficacy and safety in patients with previously treated CML.
- Other names
- relcobatinib
02
Targets
ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)
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