Drug intelligence / Profile preview

AT7519M + bortezomib

Development stage
Unknown
Lead developer
Astex Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous
01

Overview

AT7519M + bortezomib is an investigational combination therapy for the treatment of multiple myeloma, particularly in patients with relapsed or refractory disease. **AT7519M** is a potent, ATP-competitive multi-cyclin dependent kinase (CDK) inhibitor with strong activity against CDK1, CDK2, CDK4, CDK6, and especially CDK9, leading to inhibition of transcription via RNA polymerase II, cell cycle arrest, and apoptosis in tumor cells. **Bortezomib** is a reversible inhibitor of the 26S proteasome, leading to disruption of protein degradation pathways and induction of apoptosis in cancer cells. The combination has shown enhanced clinical activity, with higher response rates compared to AT7519M alone, in early-phase clinical trials for patients with advanced multiple myeloma. The maximum tolerated doses were 21 mg/m² for AT7519M and 1.3 mg/m² for bortezomib. The combination was generally well tolerated and demonstrated a 33% partial remission or better in heavily pretreated patients[1][2][5].

Other names
AT-7519M + bortezomib
02

Targets

CDK6 (Cyclin-dependent kinase 6)CDK1 (Cyclin-dependent kinase 1)CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)PSMB9 (Immunoproteasome subunit beta type-1i)CDK9 (Cyclin-dependent kinase 9)GSK3 (Glycogen synthase kinase 3 beta)CDK5 (Cyclin-dependent kinase 5)PSMB5 (Proteasome subunit beta Type-5)

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