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Other antitumour antibioticsUsed in a few countriesDerivative of an earlier drugNeeds review

Peplomycin

Also known as Pepleomycin

A derivative of bleomycin given by injection. Clinical reports from 2020 and 2022 describe its use in squamous cell carcinoma of the mouth and lip, mostly by intra-arterial infusion.

From discovery to approval

  1. 1978 · Earliest report found

    Umezawa's 1978 review describes selecting a derivative, 'bleomycin PEP', from studies of bleomycin analogues. Papers from 1983 use PEP for peplomycin and call it a derivative of bleomycin. That the 1978 compound is peplomycin is inferred from the abbreviation.[2][3][4]

  2. No approval is recorded on this site.

How it works

In two oral squamous carcinoma cell lines, peplomycin caused dose-dependent cytotoxicity and DNA laddering, with nuclear condensation in the bleomycin-sensitive line. The authors conclude that its apoptosis-inducing effect depended on each line's sensitivity to bleomycin.[1]

Where it came from and why

Umezawa's 1978 review reports studies of more useful derivatives or analogues of bleomycin. The papers cited do not state the reason for choosing this analogue; a 1983 clinical study found its lung toxicity the same as bleomycin's.

Cancers

  • Oral squamous cell carcinoma

    In a study of 141 patients with stage II to IV oral squamous cell carcinoma, preoperative intra-arterial docetaxel, cisplatin and peplomycin with intravenous fluorouracil gave a 5-year overall survival of 74.6%.[5]

  • Lip squamous cell carcinoma

    A 2022 report of 27 cases (title only) describes continuous intra-arterial peplomycin infusion for squamous cell carcinoma of the lip.[6]

  • Lung cancer

    A 1983 report used peplomycin-containing regimens in 81 patients with advanced primary lung cancer and 32 with metastatic pulmonary tumours.[4]

Family and partners

Derived from: Bleomycin

Worth knowing

  • In the 1983 report of 113 patients, definite pulmonary toxicity occurred in 7 (6.2%), six of whom died of pulmonary fibrosis, and the findings were the same as those of bleomycin lung toxicity.[4]
  • In hamsters, intraperitoneal peplomycin did not significantly raise lung hydroxyproline, while bleomycin did at the high dose; given intratracheally, both caused fibrosis, with a smaller increase for peplomycin.[7]

References

  1. Okamura H, Morimoto H, Haneji T. Peplomycin-induced apoptosis in oral squamous carcinoma cells depends on bleomycin sensitivity. Oral Oncol. 2001;37(4):379-85. PubMedDOI
  2. Umezawa H. Recent advances in antitumor antibiotics. Antibiot Chemother (1971). 1978;23:76-87. PubMed
  3. Mizuno S, Ishida A, Uehara Y, Nanjo T. Modulation of the cytotoxicity of the antitumor antibiotic peplomycin by membrane-interacting drugs and by increased levels of calcium ions. Gan. 1983;74(5):767-76. PubMed
  4. Shinkai T, Saijo N, Tominaga K, Eguchi K, Shimizu E, Shibuya M, et al. Pulmonary toxicity induced by pepleomycin 3-[(S)-1'-phenylethylamino] propylamino-bleomycin. Jpn J Clin Oncol. 1983;13(2):395-410. PubMed
  5. Hasegawa H, Kaneko T, Kanno C, Endo M, Yamazaki M, Kitabatake T, et al. Preoperative intra-arterial chemotherapy with docetaxel, cisplatin, and peplomycin combined with intravenous chemotherapy using 5-fluorouracil for oral squamous cell carcinoma. Int J Oral Maxillofac Surg. 2020;49(8):984-992. PubMedDOI
  6. Onishi M, Takahashi K, Maeda F, Akasaka T, Amano H. Successful treatment of squamous cell carcinoma on the lip with continuous intra-arterial peplomycin infusion chemotherapy: a report of 27 cases. Eur J Dermatol. 2022;32(2):287-289. PubMedDOI
  7. Yoshida A, Yamada T, Hiramatsu M, Kiuchi H, Sekiya S, Kawaguchi T, et al. Peplomycin sulfate and pulmonary fibrosis: hydroxyproline, uronic acid, proline hydroxylase and glucosamine 6-phosphate synthetase in lungs of hamsters treated with peplomycin. J Antibiot (Tokyo). 1983;36(8):1067-75. PubMedDOI