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enzastaurin + fulvestrant
- Development stage
- Phase 2
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular Injection
01
Overview
Enzastaurin + fulvestrant is a combination therapy under investigation for the treatment of hormone receptor-positive breast cancer. Enzastaurin is a small molecule protein kinase C beta (PKCβ) inhibitor, while fulvestrant is a selective estrogen receptor degrader (SERD). The rationale for combining these agents is to target both the estrogen receptor pathway and downstream signaling pathways implicated in resistance to endocrine therapy. Fulvestrant works by binding to and degrading the estrogen receptor, thereby inhibiting estrogen-dependent tumor growth. Enzastaurin inhibits PKCβ, which may help overcome resistance mechanisms in breast cancer cells[1][4].
- Other names
- enzastaurin and fulvestrantfulvestrant plus enzastaurin
02
Targets
ESR1 (ERα)ESR2 (ERβ)PRKCB (Protein kinase C beta)
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