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Table 3 Drugs targeting PI3K in clinical trial

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)

 

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

  

CUDC-907/Fimepinostat (Curis)

Rigosertib/ON-01910 (Onconova Therapeutics)

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