Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2024 Apr 22;15(11):3254-3271.
doi: 10.7150/jca.94109. eCollection 2024.

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

Affiliations
Review

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

Dimitrios Matthaios et al. J Cancer. .

Abstract

Temozolomide is an imidazotetrazine with a long history in oncology especially for the high grade malignant glioma and metastatic melanoma. However, last year's new indications for its use are added. Its optimum pharmacodynamic profile, its ability to penetrate the blood-brain barrier, the existence of methylation of MGMT in solid tumors which enhances its efficacy, the identification of new agents that can overcome temozolomide's resistance, the promising role of temozolomide in turning immune cold tumors to hot ones, are leading to expand its use in other solid tumors, giving oncologists an additional tool for the treatment of advanced and aggressive neoplasms.

Keywords: solid tumors; temozolomide.

PubMed Disclaimer

Conflict of interest statement

Competing Interests: The authors have declared that no competing interest exists.

Figures

Figure 1
Figure 1
Frequency of MGMT promoter methylation in different solid tumors. Markus Christmann et al. Bernd Kaina O(6)-Methylguanine-DNA methyltransferase (MGMT) in normal tissues and tumors: enzyme activity, promoter methylation and immunohistochemistry Biochim Biophys Acta. 2011 Dec;1816(2):179-90.
Figure 2
Figure 2
Strategies to overcome temozolomide's resistance.
Figure 3
Figure 3
Potential future role of temozolomide in turning immune “cold” tumors to “hot” ones.

Similar articles

References

    1. Middleton MR, Grob JJ, Aaronson N, Fierlbeck G, Tilgen W, Seiter S, Gore M, Aamdal S, Cebon J, Coates A, Dreno B, Henz M, Schadendorf D, Kapp A, Weiss J, Fraass U, Statkevich P, Muller M, Thatcher N. Randomized phase III study of temozolomide versus dacarbazine in the treatment of patients with advanced metastatic malignant melanoma. J Clin Oncol. 2000;18(1):158–66. - PubMed
    1. D'Atri S, Tentori L, Lacal PM, Graziani G, Pagani E, Benincasa E, Zambruno G, Bonmassar E, Jiricny J Involvement of the mismatch repair system in temozolomide-induced apoptosis. Mol Pharmacol. 1998; 54:334-341. - PubMed
    1. Danson SJ, Middleton MR. Temozolomide: a novel oral alkylating agent. Expert Rev Anticancer Ther. 2001;1:13–19. - PubMed
    1. Newlands ES, Stevens MF, Wedge SR, Wheelhouse RT, Brock C Temozolomide. a review of its discovery, chemical properties, pre-clinical development and clinical trials. Cancer Treat Rev. 1997;23:35–61. - PubMed
    1. Stevens MF, Hickman JA, Langdon SP, Chubb D, Vickers L, Stone R, Baig G, Goddard C, Gibson NW, Slack JA, Newton C, Lunt E, Fizames C, Lavelle F. Antitumor activity and pharmacokinetics in mice of 8-carbamoyl-3-methyl-imidazo[5, 1-d]-1, 2, 3, 5-tetrazin-4(3H)-one (CCRG 81045; M & B 39831), a novel drug with potential as an alternative to dacarbazine. Cancer Res. 1987;47:5846–5852. - PubMed