Clinical studies with 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037).

Paper

Clinical studies with 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037).

Published Mar 1, 1971 · H. Hansen, O. Selawry, F. Muggia

Cancer research

Q1 SJR score

101

Citations

0

Influential Citations

Semantic Scholar

Abstract

Summary The clinical tolerance to 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea was explored in patients with advanced cancer. This compound is related to 1,3-bis(2-chloroethyl)-1-nitrosourea, an agent of recognized antineoplastic effectiveness, but has only one chloroethyl group, is more lipid soluble, and is at least as active or more active against mouse Leukemia 1210. A single p.o. dose of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea was given because of the superiority of widely spaced doses against Leukemia 1210 and the expected delayed hematological toxicity. The starting dose of 15 mg/sq m body surface area corresponded to one-third of the minimal toxic dose in the most sensitive animal species in preclinical studies. Large initial increments of drug dose at presumably nontoxic levels were followed by progressively smaller dose increments to the range of moderate, reversible toxicity. Forty patients with cancer received 82 treatments. Reproducible subtoxic decrease of thrombocytes occurred at the third dose step (50 mg/sq m); decrease of leukocytes occurred at the fifth dose step (100 mg/sq m). Dose-limiting toxicity resulting in delayed thrombocytopenia and leukopenia within 4 and 6 weeks, respectively, was reached at 130 mg/sq m. This dose was well tolerated in 6 patients when given at intervals of 6 weeks. Objective responses at toxic doses were seen in 2 of 5 patients with evaluable bronchogenic carcinoma and in both patients with malignant lymphoma. Marked neurological improvement was noted in all 3 patients with glioblastoma multiforme.

Non-RCT

Highly Cited

Study Snapshot

1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea shows potential as an effective and well-tolerated treatment for advanced cancers, with potential responses in various cancer types and neurological improvement in glioblastoma multiforme patients.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Clinical studies with 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037).

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References

The absorption, distribution, excretion, and biotransformation of the carcinostatic 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea in animals.

The carcinostatic 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea rapidly degrades in mouse and dog plasma, is primarily excreted by kidneys, and is primarily bound to cyclohexyl proteins, with inactive cata

BCNU (1,3), BIS(B‐chloroethyl)‐1‐nitrosourea. Effects on advanced Hodgkin's disease and other neoplasia

BCNU shows promise as a rapid and effective treatment for advanced Hodgkin's disease, with potential for use in lymphosarcoma and reticulum cell sarcoma patients.

The physiological disposition of the carcinostatic 1,3‐bis(2‐chloroethyU‐l‐nitrosourea (BCNU) in man and animals

BCNU, an active antitumor agent, rapidly degrades and is rapidly excreted in both humans and animals, with some remaining in the bile and causing prolonged plasma levels.

Central nervous system leukemia and solid tumors of childhood: Treatment with 1,3‐bis (2‐chloroethyl)‐1‐nitrosourea (BCNU)

BCNU shows potential in treating central nervous system leukemia and solid tumors in children, with thrombocytopenia being a constant issue.

Clinical trials with 1,3-bis(2-chloroethyl)-1-nitrosourea, NSC-409962.

BCNU is a tolerable and effective anti-cancer agent with potential for use in various malignancies, with hematologic toxicity being dose-limiting and minor hepatic and renal toxicity.

MICROBIOLOGICAL EVALUATION OF 1,3-BIS (2-CHLOROETHYL)-I-NITROSOUREA.

1,3-bis (2-chloroethyl)-1-nitrosourea (NSC-409962) is a potent inhibitor of nonproliferating microorganisms with potential as an anti-leukemic agent.

Citations

Assessment of drug-loaded nanoparticles in a 3D in vitro brain tumour model

This study created a 3D in vitro brain tumor model to test novel drug delivery systems for local delivery, evaluating their selective cytotoxicity towards tumor tissue and potential benefits compared to free drug.

Principles of dose finding studies in cancer: a comparison of trial designs

Bayesian model-based and curve-free methods are preferable to algorithmic methods in Phase I cancer trials due to their superior ability to identify the dose with the desired toxicity rate and allocate patients to doses at or close to that dose.

CCNU toxicity after an overdose in a patient with Hodgkin's disease. Effects on colony-forming cells (CFU-C) and colony-stimulating activity (CSA).

CCNU overdose in a Hodgkin's disease patient led to severe bone marrow depression, but CSA-producing cells recovered earlier and were more resistant to CCNU than CFU-C cells.

Safety, Pharmacokinetics, and Efficacy of CPX-1 Liposome Injection in Patients with Advanced Solid Tumors

CPX-1 liposome injection is well-tolerated and shows antitumor activity in patients with advanced solid tumors, with a recommended dose of 210 units/m2 for future studies.

Gastrointestinal toxicity of chemotherapeutic agents.

Preventing and treating gastrointestinal toxicities in cancer chemotherapy can improve survival rates and reduce dose reductions.