Drug intelligence / Profile preview

lapatinib + metformin + niacinamide + plerixafor + temozolomide

Development stage
Unknown
Lead developer
GSK
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Subcutaneous, Oral
01

Overview

This is a combination of five drugs: lapatinib, metformin, niacinamide, plerixafor, and temozolomide. The provided search results offer detailed information about plerixafor and temozolomide. Plerixafor (brand name Mozobil) is a hematopoietic stem cell mobilizer used in combination with filgrastim to mobilize hematopoietic stem cells from the bone marrow to the bloodstream for collection and transplantation in patients with non-Hodgkin's lymphoma or multiple myeloma. It works by inhibiting the binding of stromal cell-derived factor 1 (SDF-1a/CXCL12) to its receptor CXCR4. Plerixafor is also being investigated for treating glioblastoma, where it may prevent recurrence by inhibiting vasculogenesis. Temozolomide is an alkylating agent used to treat certain types of brain tumors, particularly glioblastoma multiforme and refractory anaplastic astrocytoma. It is a prodrug that requires nonenzymatic hydrolysis to perform alkylation of adenine/guanine residues, leading to DNA damage and eventual cell death. The search results mention clinical trials and a case report investigating a combination of plerixafor and temozolomide for glioblastoma, often as part of chemo-radiotherapy. However, information about lapatinib, metformin, and niacinamide is not present in the provided search results, and this specific five-drug combination is not directly addressed.

02

Targets

GSEC (Gamma-Secretase Complex)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)SIRT (Sirtuin family)CXCR4 (C-X-C motif chemokine receptor 4)DNAND1 (Mitochondrial electron transport chain complex I)

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