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Drug intelligence / Profile preview
Serabelisib + sapanisertib
- Development stage
- Phase 2
- Lead developer
- Faeth Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Serabelisib + sapanisertib is an investigational fixed-dose oral combination therapy developed by Faeth Therapeutics for the treatment of endometrial cancer and other solid tumors. The combination targets the PI3K/AKT/mTOR pathway—a key oncogenic and metabolic signaling axis frequently mutated in cancer—by simultaneously inhibiting PI3K-alpha (serabelisib) and both mTORC1 and mTORC2 complexes (sapanisertib). This dual blockade aims to achieve more complete pathway inhibition than single agents, potentially overcoming resistance mechanisms such as those seen with taxane chemotherapy. Preclinical studies have shown that this combination enhances cytotoxicity when used with paclitaxel. Early-phase clinical trials have demonstrated promising efficacy and tolerability in patients with advanced or recurrent endometrial, ovarian, breast cancers and other solid tumors[1][4][5][6].
- Brand names
- PIKTOR
- Other names
- serabelisib + sapanisertibsapanisertib/serabelisib
02
Targets
Mechanistic target of rapamycin complex 1Mechanistic target of rapamycin kinase complex 2PIK3CA (Phosphoinositide 3-kinase alpha)
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