. Topotecan and belotecan are camptothecin derivatives that are used to treat small cell lung cancer (SCLC). This study compared the toxicities and efficacies of belotecan and topotecan monotherapies in patients with SCLC. . We retrospectively reviewed data from 94 patients with SCLC (with or without prior chemotherapy) who were treated using belotecan monotherapy ( = 59, 188 cycles) or topotecan monotherapy ( = 35, 65 cycles) between September 2003 and December 2011. . Thrombocytopenia occurred during 42% and 61.5% of the belotecan and topotecan cycles, respectively ( = 0.007). Significant differences between belotecan and topotecan were also observed for grade 4/5 lung infection (3.2% versus 10.8%, resp.; = 0.003), all-grade headache (3.2% versus 10.8%, resp.; = 0.017), and grade 4/5 increased liver enzymes (0.5% versus 4.6%, resp.; = 0.023). The median TTPDs, CSSs, and OSs were 14 months and 11.6 months ( = 0.646), 10 months and 7 months ( = 0.179), and 34.5 months and 21.4 months ( = 0.914) after belotecan and topotecan monotherapy, respectively. . Belotecan monotherapy may be safer than topotecan monotherapy in SCLC patients. And in terms of efficacy, belotecan could be comparable to topotecan monotherapy.
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http://dx.doi.org/10.1155/2016/3576201 | DOI Listing |
Front Oncol
March 2023
Department of Thoracic Surgery, Fudan University Affiliated Huadong Hospital, Shanghai, China.
Molecules
February 2023
Institut de Chimie Pharmaceutique Albert Lespagnol (ICPAL), Faculté de Pharmacie, University of Lille, 3 rue du Professeur Laguesse, BP-83, F-59006 Lille, France.
The antitumor drug topotecan (TPT) is a potent inhibitor of topoisomerase I, triggering DNA breaks lethal for proliferating cancer cells. The mechanism is common to camptothecins SN38 (the active metabolite of irinotecan) and belotecan (BLT). Recently, TPT was shown to bind the ribosomal protein L15, inducing an antitumor immune activation independent of topoisomerase I.
View Article and Find Full Text PDFExpert Opin Drug Discov
June 2022
Departamento de Química Orgánica I - Centro de Investigación Lascaray, Facultad de Farmacia, Universidad del País Vasco, Paseo de la Universidad 7, 01006 Vitoria, Spain.
Introduction: Cancer has been identified as one of the leading causes of death worldwide. The biological target of some anticancer agents is topoisomerase I, an enzyme involved in the relaxation of supercoiled DNA. The synthesis of new compounds with antiproliferative effect and behaving as topoisomerase I inhibitors has become an active field of research.
View Article and Find Full Text PDFEur J Med Chem
November 2021
College of Pharmacy, University of Sharjah, 27272, Sharjah, United Arab Emirates; Sharjah Institute for Medical Research, 27272, Sharjah, United Arab Emirates. Electronic address:
Nature represents a rich source of compounds used for the treatment of many diseases. Camptothecin (CPT), isolated from the bark of Camptotheca acuminata, is a cytotoxic alkaloid that attenuates cancer cell replication by inhibiting DNA topoisomerase 1. Despite its promising and wide spectrum antiproliferative activity, its use is limited due to low solubility, instability, acquired tumour cell resistance, and remarkable toxicity.
View Article and Find Full Text PDFJ Thorac Dis
October 2020
Department of Medical Oncology, Tata Memorial Hospital, Parel, Mumbai; Homi Bhabha National Institute, Mumbai, India.
Systemic treatment in small cell lung carcinoma has been a challenge for oncologists for decades. The high propensity for recurrence is usually due to distant metastasis, which makes systemic treatment an essential component of treatment in small cell lung carcinoma. The regimen of cisplatin and etoposide (established in the mid-1980's) concurrently with thoracic radiotherapy followed by prophylactic cranial irradiation (PCI) remains the standard of care in limited stage disease.
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