Temozolomide: a novel oral alkylating agent

doi:10.1586/14737140.1.1.13

Paper

Temozolomide: a novel oral alkylating agent

Published Jun 1, 2001 · S. Danson, M. Middleton

Expert Review of Anticancer Therapy

Q2 SJR score

106

Citations

5

Influential Citations

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Abstract

Temozolomide is an imidazotetrazine with a mechanism of action and efficacy similar to dacarbazine (DTIC). However, it differs from DTIC in that it can be taken orally, degrades spontaneously to an active metabolite and penetrates the blood–brain barrier. It is well tolerated, making it a suitable candidate for combination chemotherapy. Trials to date have focussed on its activity in advanced metastatic melanoma and high-grade malignant glioma. Investigations into other indications, in particular solid tumors with central nervous system metastases, are ongoing. Studies of new drug schedules and of drugs to ameliorate temozolomide resistance offer the prospect of increased efficacy.

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Study Snapshot

Temozolomide is a promising oral alkylating agent for treating advanced metastatic melanoma and high-grade malignant glioma, with potential for combination chemotherapy in other solid tumors with central nervous system metastases.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Temozolomide: a novel oral alkylating agent

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References

O6‐methylguanine formation, repair protein depletion and clinical outcome with a 4 hr schedule of temozolomide in the treatment of advanced melanoma: Results of a phase II study

A 4-hour schedule of temozolomide shows activity against advanced melanoma, with greater MGMT depletion and O6-methylguanine formation than previously reported for O6-alkylating agent regimens.

Schedule-dependent activity of temozolomide plus CPT-11 against a human central nervous system tumor-derived xenograft.

The combination of temozolomide and CPT-11 shows schedule-dependent enhancement of antitumor activity against a malignant glioma-derived xenograft, suggesting potential for a Phase I trial.

A phase II study of temozolomide vs. procarbazine in patients with glioblastoma multiforme at first relapse

TMZ significantly improves progression-free survival and overall survival compared to procarbazine in patients with glioblastoma multiforme at first relapse, with a better quality of life.

Post hoc economic analysis of temozolomide versus dacarbazine in the treatment of advanced metastatic melanoma.

Oral temozolomide shows a survival trend favoring it over intravenous dacarbazine for metastatic melanoma, but its cost-effectiveness is comparable to many interventions due to differences in convenience and costs.

Temozolomide, a novel alkylating agent with activity in the central nervous system, may improve the treatment of advanced metastatic melanoma.

Temozolomide shows promise in treating central nervous system malignancies, including advanced metastatic melanoma, with a similar safety profile and lower incidence of central nervous system relapse compared to dacarbazine.

Citations

Calnexin promotes glioblastoma progression by inducing protective mitophagy through the MEK/ERK/BNIP3 pathway

Calnexin (CANX) overexpression in glioblastoma cells promotes progression by inducing protective mitophagy through the MEK/ERK/BNIP3 pathway, potentially identifying a therapeutic target for GBM treatment.

Revisiting Temozolomide's role in solid tumors: Old is gold?

Temozolomide's effectiveness in treating advanced and aggressive solid tumors has expanded, offering oncologists an additional tool for treating advanced and aggressive neoplasms.

Temozolomide, Procarbazine and Nitrosoureas in the Therapy of Malignant Gliomas: Update of Mechanisms, Drug Resistance and Therapeutic Implications

Temozolomide, procarbazine, and nitrosoureas effectively treat malignant gliomas, but resistance mechanisms exist, and alternative therapies are needed to overcome chemoresistance.

An Overview of Nanotherapeutic Drug Delivery Options for the Management of Glioblastoma

Nanoparticle formulations show promise in overcoming the blood-brain barrier for effective glioma treatment, but need further clinical translation and overcome pitfalls.

Methadone Potentiates the Cytotoxicity of Temozolomide by Impairing Calcium Homeostasis and Dysregulation of PARP in Glioblastoma Cells

Methadone can increase the cytotoxicity of temozolomide in glioblastoma cells by impairing calcium homeostasis and dysregulating PARP-1 protein, without affecting opioid receptors.