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Cyclophosphamide

Laurance V. Foye

Open publisher page 14 citations

Abstract

Cyclophosphamide (2H-1, 3, 2-oxazaphosphorine, 2-[bis(2-chloroethyl) amino] tetrahydro-2-oxide) was developed in the search for an inactive "transport" form of the β-chloroethyl group of alkylating compounds. Studies have shown that this compound is relatively inactive in vitro and is converted to the active form in vivo.1-3Trials in various tumor-bearing animals confirmed this in vivo activity and demonstrated fairly potent antitumor effect.1-5 Preliminary studies in humans suggested that this compound possessed a spectrum of antitumor activity similar to that of other nitrogen mustards, but that it was considerably less toxic.6,7 We have conducted a brief clinical trial of this agent* in a small group of patients with advanced malignancies. This study was not intended to be definitive but was designed to give some indications as to the effective dosage levels and routes, and types and degree of toxicity of cyclophosphamide as compared with the more familiar alkylating agents. Seven

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What this paper is about

Cyclophosphamide (2H-1, 3, 2-oxazaphosphorine, 2-[bis(2-chloroethyl) amino] tetrahydro-2-oxide) was developed in the search for an inactive "transport" form of the β-chloroethyl group of alkylating compounds. Studies have shown that this compound is relatively inactive in vitro and is converted to the active form in vivo.1-3Trials in various tumor-bearing animals confirmed this in vivo activity and demonstrated fairly potent antitumor effect.1-5 Preliminary studies in humans suggested that this compound possessed a spectrum of antitumor activity similar to that of other nitrogen mustards, but that it was considerably less toxic.6,7 We have conducted a brief clinical trial of this agent* in a small group of patients with advanced malignancies. This study was not intended to be definitive but was designed to give some indications as to the effective dosage levels and routes, and types and degree of toxicity of cyclophosphamide as compared with the more familiar alkylating agents. Seven

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Available abstract

Cyclophosphamide (2H-1, 3, 2-oxazaphosphorine, 2-[bis(2-chloroethyl) amino] tetrahydro-2-oxide) was developed in the search for an inactive "transport" form of the β-chloroethyl group of alkylating compounds. Studies have shown that this compound is relatively inactive in vitro and is converted to the active form in vivo.1-3Trials in various tumor-bearing animals confirmed this in vivo activity and demonstrated fairly potent antitumor effect.1-5 Preliminary studies in humans suggested that this compound possessed a spectrum of antitumor activity similar to that of other nitrogen mustards, but that it was considerably less toxic.6,7 We have conducted a brief clinical trial of this agent* in a small group of patients with advanced malignancies. This study was not intended to be definitive but was designed to give some indications as to the effective dosage levels and routes, and types and degree of toxicity of cyclophosphamide as compared with the more familiar alkylating agents. Seven

Key concepts: Cyclophosphamide, In vivo, Nitrogen mustard, Toxicity, In vitro, Pharmacology, Chemistry, Chemotherapy

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