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  Mechlorethamine Gel

Mechlorethamine is  a nitrogen mustard and an analogue of sulfur mustard, with antineoplastic and immunosuppressive activities. Mechlorethamine is metabolized to an unstable, highly reactive ethyleniminium intemediate that alkylates DNA, particularly the 7 nitrogen of guanine residues, resulting in DNA base pair mismatching, DNA interstrand crosslinking, the inhibition of DNA repair and synthesis, cell-cycle arrest, and apoptosis. This agent also exhibits lympholytic properties. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Successful clinical use of mechlorethamine gave birth to the field of anticancer chemotherapy. The drug is an nitrogen-based analogue of mustard gas (which is sulfur-based) and was derived from chemical warfare research. Secret clinical trials of the agent for Hodgkin's disease and several other lymphomas and leukemias in humans began in December 1942. Because of wartime secrecy restrictions, it was not until 1946 that the results of these trials were published openly.(source: http://en.wikipedia.org/wiki/Mechlorethamine).

Mechlorethamine gel is Yaupon’s investigational, proprietary topical formulation of mechlorethamine. Mechlorethamine is a chemotherapeutic agent previously approved for intravenous treatment of mycosis fungoides, the most common type of CTCL. Topical mechlorethamine preparations are recommended for treatment of early stage CTCL by the National Comprehensive Cancer Network (NCCN)*. However, there are no FDA-approved topical mechlorethamine drugs, limiting its availability to non-standardized, pharmacist-compounded preparations. These preparations are typically either aqueous- or paraffin- (petroleum jelly) based formulations. Paraffin-based formulations are extremely greasy and inconvenient. Yaupon’s proprietary mechlorethamine gel is a novel formulation that has been standardized and made under Good Manufacturing Practices (GMPs). A pivotal multi-center clinical study of this topical mechlorethamine gel in patients with early stage mycosis fungoides, a type of CTCL, met its primary and secondary endpoints. The primary endpoint was an assessment of lesion severity. Adverse events potentially related to Yaupon’s formulation include dermatitis (skin irritation, pruritus and erythema) and hyperpigmentation. Dermatitis ranged from mild to moderately severe. Based on these results, Yaupon submitted a New Drug Application (NDA) to the FDA in July 2011. Yaupon’s mechlorethamine gel has been granted Fast Track Status and Orphan Drug Status by the FDA. (source: http://www.yaupontherapeutics.com/investigational_drug/default.asp).

Current developer:   Yaupon Therapeutics

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