VNP40101M is a novel alkylating agent that has been used in trials studying the treatment of Leukemia, Lymphoma, Lung Cancer, Small Intestine Cancer, and Myelodysplastic Syndromes, among others.
- Mechanism
- Curator reviewed
VNP40101M is a small molecule that works by damaging DNA. It releases the DNA chloroethylating agent 90CE after entering the blood stream. 90CE chloroethylates the O6 position of guanine residues, ultimately resulting in an interstrand DNA cross-link. Interstrand DNA cross-links are difficult to repair and are toxic to cells. VNP40101M demonstrates a broad spectrum of anticancer activity in preclinical studies, including activity in selected cell lines resistant to other alkylating agents such as BCNU, cyclophosphamide and melphalan. In preclinical studies, Cloretazine (VNP40101M) has been combined with other anticancer agents such as cytarabine (Ara-C). In addition, Cloretazine (VNP40101M) or its metabolite, has been shown to be capable of crossing the blood brain barrier in preclinical models.
- Primary indication
- Investigated for use/treatment in brain cancer, cancer/tumors (unspecified), colorectal cancer, leukemia (lymphoid), leukemia (myeloid), lung cancer, myelodysplastic syndrome, pediatric indications, and solid tumors.Curator reviewed
- Formula / weight
- C6H14ClN3O5S2 · 307.775 g/mol (avg)
- Also known as
- Cloretazine · Onrigin
- Code names
- 101M · VNP-40101M
Resolves to
PVCULFYROUOVGJ-UHFFFAOYSA-NSMILESCNC(=O)N(N(CCCl)S(C)(=O)=O)S(C)(=O)=OWhat you can answer from here — as of July 03, 2026
Which drugs share a target with Laromustine, and which of those have an active Phase 3 trial?
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