Drug intelligence / Profile preview

afuresertib

Development stage
Phase 3
Lead developer
Laekna
Modality
Small Molecules
Administration
Oral
01

Overview

Afuresertib is an orally bioavailable, small-molecule inhibitor of the serine/threonine protein kinase Akt (also known as protein kinase B or PKB). It acts as a pan-AKT inhibitor, targeting all three isoforms of AKT. By inhibiting AKT activity, afuresertib disrupts the PI3K/Akt signaling pathway, which is frequently dysregulated in cancer and associated with tumorigenesis, cell proliferation, survival, and resistance to antineoplastic agents. Preclinical studies have shown that afuresertib can reverse platinum resistance in ovarian cancer cell lines. Clinically, it has demonstrated anti-cancer activity and a tolerable safety profile in multiple solid tumors and hematologic malignancies. Afuresertib has been investigated both as monotherapy and in combination with other therapies (e.g., fulvestrant) for various cancers including breast cancer (HR+/HER2-, triple-negative), ovarian cancer (including platinum-resistant), prostate cancer, gastric cancer, multiple myeloma, chronic lymphocytic leukemia, histiocytosis, and other solid tumors[1][2][3][4][5][6][7].

Other names
Afuresertib hydrochloride
02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)

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