Drug intelligence / Profile preview

melphalan + carfilzomib + thalidomide + cisplatin + doxorubicin + cyclophosphamide + etoposide

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

Overview

This is a multi-agent chemotherapy regimen composed of seven drugs—melphalan, carfilzomib, thalidomide, cisplatin, doxorubicin, cyclophosphamide, and etoposide—used primarily in the treatment of multiple myeloma and other aggressive hematologic malignancies. Each component has a distinct mechanism of action: - Melphalan and cyclophosphamide are alkylating agents that crosslink DNA strands to inhibit cancer cell replication. - Carfilzomib is a proteasome inhibitor that disrupts protein degradation pathways in malignant plasma cells. - Thalidomide is an immunomodulatory drug with antiangiogenic properties. - Cisplatin forms DNA adducts leading to apoptosis. - Doxorubicin intercalates into DNA and inhibits topoisomerase II activity. - Etoposide inhibits topoisomerase II as well, causing double-strand breaks in DNA. This combination is used for rapid cytoreduction in high-risk or relapsed/refractory multiple myeloma patients. It may be referred to as an intensive salvage or induction regimen prior to autologous stem cell transplantation[2][4][6][7].

02

Targets

PSMB5 (Proteasome subunit beta Type-5)CRBN (Cereblon)TOP2A (DNA topoisomerase II)DNA

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