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Drug intelligence / Profile preview
lerociclib
- Development stage
- Phase 3
- Lead developer
- G1 Therapeutics
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Lerociclib is an orally bioavailable small molecule inhibitor of cyclin-dependent kinase 4 (CDK4) and cyclin-dependent kinase 6 (CDK6), developed primarily for the treatment of hormone receptor-positive (HR+), HER2-negative advanced or metastatic breast cancer. It acts by selectively inhibiting CDK4/6 activity, thereby blocking cell cycle progression from the G1 to S phase in tumor cells dependent on this pathway. Lerociclib has demonstrated antineoplastic activity and a differentiated safety profile in clinical trials. It is being investigated both as monotherapy and in combination with endocrine therapies such as fulvestrant or letrozole[2][3][9][10].
- Other names
- G1T38 free baseG-1T38 free baseG 1T38 free base
02
Targets
P-TEFb (Positive transcription elongation factor b)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)
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