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Drug intelligence / Profile preview
abemaciclib + lasofoxifene
- Development stage
- Phase 3
- Lead developer
- Sermonix Pharmaceuticals
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Abemaciclib + lasofoxifene is an investigational oral combination therapy for the treatment of estrogen receptor–positive (ER+), human epidermal growth factor receptor 2–negative (HER2-) metastatic breast cancer with acquired resistance due to ESR1 mutations. Abemaciclib is a small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in cancer cells. Lasofoxifene is a selective estrogen receptor modulator (SERM) that antagonizes mutant forms of the estrogen receptor alpha, particularly those harboring ESR1 mutations that confer resistance to standard endocrine therapies. The combination aims to overcome endocrine resistance and improve clinical outcomes in patients who have progressed after prior endocrine therapy and CDK4/6 inhibitors[3][4][9].
- Other names
- abemaciclib + lasofoxifene
02
Targets
CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)ESR1 (ERα)
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