Drug intelligence / Profile preview

afuresertib + carfilzomib

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**afuresertib + carfilzomib** is an experimental combination therapy used primarily in research for the treatment of relapsed/refractory multiple myeloma. - **Afuresertib** is an oral, small molecule inhibitor of AKT, a key kinase in the PI3K/AKT pathway that is constitutively active in many hematologic malignancies, promoting cell survival and drug resistance. By inhibiting AKT, afuresertib induces apoptosis and suppresses proliferation in tumor cells[2]. - **Carfilzomib** is a selective, irreversible inhibitor of the 20S proteasome, the proteolytic core particle of the 26S proteasome. This leads to accumulation of polyubiquitinated proteins, resulting in cell cycle arrest and apoptosis, particularly in multiple myeloma cells[1][3]. The combination is being investigated for possible synergistic antimyeloma effects, given the distinct but complementary mechanisms of action of each agent. Early clinical investigations suggest the combination is under study in relapsed/refractory multiple myeloma[2].

02

Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)PSMB2 (Proteasome subunit beta type-2)PSMB5 (Proteasome subunit beta Type-5)

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