Drug intelligence / Profile preview

lomustine + methylprednisone + vincristine

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three drugs: - Lomustine, an alkylating nitrosourea agent that cross-links DNA and RNA, leading to inhibition of DNA and RNA synthesis and cell death. It is cell cycle–phase nonspecific and primarily used in the treatment of brain tumors and as part of combination regimens for refractory or relapsed Hodgkin's disease[4]. - Methylprednisone (more commonly referred to as methylprednisolone), a synthetic glucocorticoid corticosteroid with anti-inflammatory, immunosuppressive, and antitumor properties. It acts by binding to glucocorticoid receptors, modulating gene expression, suppressing immune responses, reducing inflammation, and inducing apoptosis in certain cancer cells. - Vincristine, a vinca alkaloid that inhibits microtubule formation in mitotic spindle fibers during cell division (M phase), resulting in metaphase arrest. It is widely used for various hematologic malignancies including acute lymphoblastic leukemia (ALL), lymphomas, Wilms' tumor, neuroblastoma, rhabdomyosarcoma[5]. This specific three-drug combination has been studied as an adjuvant chemotherapy regimen for childhood high-grade astrocytoma following surgery and radiotherapy[7]. The mechanism involves synergistic cytotoxic effects on rapidly dividing cancer cells through distinct but complementary pathways.

02

Targets

TUBB (Tubulin (alpha and beta subunits))GR (Glucocorticoid receptor)DNA

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