Drug intelligence / Profile preview

ixazomib + clarithromycin

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

I**xazomib + clarithromycin** is an investigational, orally-administered combination regimen evaluated primarily in the context of treatment for relapsed or refractory multiple myeloma. **Ixazomib** is a small molecule oral proteasome inhibitor that induces apoptosis in myeloma cells by blocking the 20S proteasome, leading to the accumulation of polyubiquitinated proteins and cancer cell death. **Clarithromycin** is a macrolide antibiotic with observed anti-myeloma and immunomodulatory activity, which may include suppression of interleukin-6 and tumor necrosis factor-alpha, and increases dexamethasone exposure by inhibiting hepatic clearance. The combination takes advantage of their complementary mechanisms—proteasome inhibition and immunomodulation—and is entirely oral, aimed at maximizing convenience and efficacy for patients with advanced disease.

02

Targets

PSMB2 (Proteasome subunit beta type-2)PSMB5 (Proteasome subunit beta Type-5)PSMB1 (26S Proteasome (β1-Subunit))CYP1A2 (Cytochrome P450 1A2)CYP3A4 (Cytochrome P450 3A4)Bacterial 50S ribosomal subunit

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