Table 1. A peek at PI3K inhibitors. According to a study in Nature by Ali et al., inhibition of phosphoinositide 3-kinase-d (PI3Kd) or the PI3K catalytic subunit d-polypeptide (PI3KCD; p110d) could treat solid tumors by modulating T cell responses. At least 12 companies are developing PI3Kd-specific inhibitors or dual PI3Kg and PI3Kd inhibitors for hematological malignancies, autoimmune disease and inflammation that could be repurposed to treat solid cancers.

Source: BCIQ: BioCentury Online Intelligence

Company

Product

Description

Status

Gilead Sciences Inc. (NASDAQ:GILD)

Idelalisib

Small molecule inhibitor of PI3Kd

In registration for chronic lymphocytic leukemia (CLL) and non-Hodgkin's lymphoma (NHL)

Takeda Pharmaceutical Co. Ltd. (Tokyo:4502)/Infinity Pharmaceuticals Inc. (NASDAQ:INFI)

IPI-145

Oral inhibitor of PI3Kg and PI3Kd

Phase III for CLL; Phase II for NHL, lymphoma, rheumatoid arthritis (RA) and inflammation; Phase I for hematological malignancies and autoimmune diseases

Rhizen Pharmaceuticals S.A./TG Therapeutics Inc. (NASDAQ:TGTX)

TGR-1202

PI3Kd inhibitor

Phase I/II for CLL, B cell lymphoma and hematological malignancies

Amgen Inc. (NASDAQ:AMGN)

AMG 319

Small molecule inhibitor of PI3Kd

Phase I for hematological malignancies

Incyte Corp. (NASDAQ:INCY)

INCB40093

PI3Kd inhibitor

Phase I for B cell lymphoma

Gilead Sciences

GS-9820

PI3Kd inhibitor

Phase I for lymphoma

Rhizen Pharmaceuticals

RP6530

Dual PI3Kg and PI3Kd inhibitor

Phase I for hematological malignancies; preclinical for B cell lymphoma and T cell lymphoma

RP6503

Dual PI3Kg and PI3Kd inhibitor

Preclinical for asthma, chronic obstructive pulmonary disease, idiopathic pulmonary fibrosis and inflammation

Exelixis Inc. (NASDAQ:EXEL)/Merck & Co. Inc. (NYSE:MRK)

XL499

Selective inhibitor of PI3Kd

Preclinical for cancer and inflammation

Pathway Therapeutics Inc./MEI Pharma Inc. (NASDAQ:MEIP)

PWT143

PI3Kd inhibitor

Preclinical for cancer

Xcovery Holding Co. LLC

X-339

Selective inhibitor of the p110d isoform of PI3K

Preclinical for CLL