Drug intelligence / Profile preview

carfilzomib + melphalan + prednisone

Development stage
Unknown
Lead developer
Amgen
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous (carfilzomib), Oral (melphalan, Prednisone)
01

Overview

This is a **combination regimen** consisting of three agents: - **Carfilzomib** is a selective, irreversible proteasome inhibitor (20S core particle of the 26S proteasome), leading to accumulation of polyubiquitinated proteins and apoptosis in malignant plasma cells. - **Melphalan** is an alkylating agent that induces DNA cross-linking, preventing DNA replication and RNA transcription, resulting in cell death, particularly in rapidly dividing cells. - **Prednisone** is a synthetic glucocorticoid corticosteroid that induces apoptosis in lymphoid cells and modulates inflammation and immune response. This specific combination is used for **multiple myeloma**, particularly for elderly or transplant-ineligible patients, and was studied in randomized clinical trials such as CLARION to compare efficacy and safety with the established bortezomib-containing regimens[3][4][5][6]. Carfilzomib is developed by Amgen and is marketed as Kyprolis[1][2][5][6]. Melphalan is manufactured under brand names such as Alkeran, originally by GSK, now produced by Aspen. Prednisone is produced as a generic product by numerous manufacturers. As of 2019, Kyprolis (carfilzomib) in combination with melphalan and prednisone was not approved by FDA for newly diagnosed transplant-ineligible multiple myeloma patients[6].

Brand names
Kyprolis + Alkeran + generic prednisone
Other names
KMPcarfilzomib-melphalan-prednisone
02

Targets

GR (Glucocorticoid receptor)DNA26S proteasome

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