From: Targeting PI3K in cancer: mechanisms and advances in clinical trials
Compound | Terminated | Phase I | Phase II | Phase III | FDA approved |
---|---|---|---|---|---|
Dual PI3K/mTOR inhibitor | BGT-226 (Novartis) DS-7423 (Daiichi Sankyo) PF-04691502 (Pfizer) PKI-179 (Pfizer) | GSK458/Omipalisib(GlaxoSmithKline) P7170 (Piramal) SB2343/VS-5584 (Verastem) | BEZ235/Dactolisib (Novartis) GDC-0084 (Novogen) GDC-0980/Apitolisib (Genentech) LY3023414 (Eli Lilly) PQR309/Bimiralisib (PIQUR Therapeutics) XL765/Voxtalisib (Sanofi) SF-1126 (SignalRx) | PF-05212384/gedatolisib/ PKI-587 (Pfizer) | Â |
Pan-PI3K inhibitor | GDC-0941/Pictilisib (Genentech) PX-866 (Oncothyreon) TG100–115 (Sanofi) | CH5132799 (TohokuNiproPharm) | XL147/ Pilaralisib (Sanofi) ZSTK474 (Zenyaku Kogyo) | BKM-120/Buparlisib (Novartis) | BAY80–6946/ Copanlisib (Bayer) |
Isoform-specific PI3K inhibitor | AZD8835 (AstraZeneca) δ/α WX-037 (Wilex) α | AZD8186 (AstraZeneca) β/δ KA2237 (Karus Therapeutics) β/δ GS-9820/CAL-120 (Gilead) β/δ ME401/PWT-143 (MEI Pharma) δ | AMG 319 (Amgen) δ GSK2636771 (GlaxoSmithKline) β INCB050465/Parsaclisib (Incyte) δ Serabelisib/INK-1117 (Takeda) α Umbralisib/TGR-1202 (TG Therapeutics) δ RP6530/Tenalisib(Rhizen Pharmaceuticals) δ/γ | GDC-0032/Taselisib (Genentech) α/δ/γ BYL719/Alpelisib (Novartis) α | Duvelisib/IPI-145 (Infinity) δ/γ CAL-101/idelalisib (Gilead) δ |
Others | Â | Â | CUDC-907/Fimepinostat (Curis) | Rigosertib/ON-01910 (Onconova Therapeutics) | Â |