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capivasertib + enzalutamide
- Development stage
- Phase 2
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**Capivasertib + enzalutamide** is a combination therapy of two small molecule drugs developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). **Capivasertib** is an orally active pan-AKT inhibitor that blocks the activity of AKT kinases, which are central components of the PI3K/AKT/mTOR pathway, often activated by loss of PTEN in prostate cancer. **Enzalutamide** is an oral androgen receptor antagonist that inhibits androgen receptor signaling, essential for prostate cancer cell survival and proliferation. The combination targets dual resistance mechanisms in mCRPC with PTEN loss or PI3K/AKT pathway aberrations, aiming to improve outcomes after progression on prior androgen-targeted therapies like abiraterone and docetaxel. Capivasertib is developed by AstraZeneca, and enzalutamide by Pfizer/Astellas. Clinical studies (phase I and II) have demonstrated that the combination is generally well tolerated, with antitumor activity in patients harboring aberrations in PI3K/AKT/mTOR, although no statistically significant improvement over enzalutamide monotherapy was established in abiraterone-pre-treated mCRPC[1][2][5][6].
- Other names
- capivasertib + enzalutamide
02
Targets
AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)AKT2 (Rac-beta serine/threonine-protein kinase)AKT3 (RAC-gamma serine/threonine-protein kinase)AR (Adrenergic receptors)
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