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287 results

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Page 1
Antibody-drug conjugates targeting TROP-2 and incorporating SN-38: A case study of anti-TROP-2 sacituzumab govitecan.
Goldenberg DM, Sharkey RM. Goldenberg DM, et al. MAbs. 2019 Aug/Sep;11(6):987-995. doi: 10.1080/19420862.2019.1632115. Epub 2019 Jul 18. MAbs. 2019. PMID: 31208270 Free PMC article. Review.
Antibody-drug conjugates (ADCs) that exploit the active metabolite SN-38, which is derived from the popular anticancer drug, irinotecan (a camptothecin that inhibits the nuclear topoisomerase I enzyme, inducing double-stranded DNA breaks during the mitotic S- …
Antibody-drug conjugates (ADCs) that exploit the active metabolite SN-38, which is derived from the popular anticancer drug, …
Irinotecan.
[No authors listed] [No authors listed] 2025 Jan 15. Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. 2025 Jan 15. Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. PMID: 29999936 Free Books & Documents. Review.
Limited data indicate that irinotecan is found in breastmilk for 2 days and its active metabolite is found in breastmilk for up to a week after a dose of 60 mg/square meter, although the highest amounts occur during the first 4 days after a dose. ...Based on this limited e …
Limited data indicate that irinotecan is found in breastmilk for 2 days and its active metabolite is found in breastmilk for up to a …
Rubitecan.
Clark JW. Clark JW. Expert Opin Investig Drugs. 2006 Jan;15(1):71-9. doi: 10.1517/13543784.15.1.71. Expert Opin Investig Drugs. 2006. PMID: 16370935 Review.
A more acidic environment favours the lactone ring structure, whereas neutral or basic conditions favour the conversion to the carboxylic acid form. In addition to issues of lactone ring stability at physiological pH (true for all of the camptothecin analogues), the …
A more acidic environment favours the lactone ring structure, whereas neutral or basic conditions favour the conversion to the carbox …
Kinetics of the in vivo interconversion of the carboxylate and lactone forms of irinotecan (CPT-11) and of its metabolite SN-38 in patients.
Rivory LP, Chatelut E, Canal P, Mathieu-Boué A, Robert J. Rivory LP, et al. Cancer Res. 1994 Dec 15;54(24):6330-3. Cancer Res. 1994. PMID: 7987823
The kinetics of the in vivo interconversion of the carboxylate and lactone forms of the prodrug irinotecan, 7-ethyl-10-[4-(1-piperidino)-1- piperidino]carbonyloxycamptothecin (CPT-11), and its active metabolite SN-38 were studied in five patients using …
The kinetics of the in vivo interconversion of the carboxylate and lactone forms of the prodrug irinotecan, 7-ethyl-10-[4-(1-p …
Addition of temsirolimus to chemotherapy in children, adolescents, and young adults with intermediate-risk rhabdomyosarcoma (ARST1431): a randomised, open-label, phase 3 trial from the Children's Oncology Group.
Gupta AA, Xue W, Harrison DJ, Hawkins DS, Dasgupta R, Wolden S, Shulkin B, Qumseya A, Routh JC, MacDonald T, Feinberg S, Crompton B, Rudzinski ER, Arnold M, Venkatramani R. Gupta AA, et al. Lancet Oncol. 2024 Jul;25(7):912-921. doi: 10.1016/S1470-2045(24)00255-9. Lancet Oncol. 2024. PMID: 38936378 Free PMC article. Clinical Trial.
We aimed to compare event-free survival in patients with intermediate-risk rhabdomyosarcoma treated with vincristine, actinomycin, and cyclophosphamide alternating with vincristine and irinotecan (VAC/VI) combined with temsirolimus followed by maintenance therapy versus VA …
We aimed to compare event-free survival in patients with intermediate-risk rhabdomyosarcoma treated with vincristine, actinomycin, and cyclo …
Involvement of specific transport system on uptake of lactone form of SN-38 in human intestinal epithelial cell line Caco-2.
Ueno Y, Matsuda H, Mizutani H, Iwamoto T, Okuda M. Ueno Y, et al. Biol Pharm Bull. 2012;35(1):54-8. doi: 10.1248/bpb.35.54. Biol Pharm Bull. 2012. PMID: 22223337 Free article.
The aim of this study was to elucidate the characteristics of the transport of lactone and carboxylate forms of SN-38 (SN-38L and SN-38C, respectively), a metabolite of irinotecan hydrochloride (CPT-11), with the human intestinal epithelial cell …
The aim of this study was to elucidate the characteristics of the transport of lactone and carboxylate forms of SN-38 ( …
The transformation of irinotecan (CPT-11) to its active metabolite SN-38 by human liver microsomes. Differential hydrolysis for the lactone and carboxylate forms.
Haaz MC, Rivory LP, Riché C, Robert J. Haaz MC, et al. Naunyn Schmiedebergs Arch Pharmacol. 1997 Aug;356(2):257-62. doi: 10.1007/pl00005049. Naunyn Schmiedebergs Arch Pharmacol. 1997. PMID: 9272733
At all concentrations of CPT-11, the steady-state velocity of SN-38 formation as well as the intercept concentrations of SN-38 were about 2-fold higher when the substrate was under the lactone form than under the carboxylate form. ...We conclude …
At all concentrations of CPT-11, the steady-state velocity of SN-38 formation as well as the intercept concentrations of SN …
Albumin-based nanoparticles encapsulating SN-38 demonstrate superior antitumor efficacy compared to irinotecan.
Xiong G, Li S, Schätzlein AG, Uchegbu IF. Xiong G, et al. Drug Deliv. 2025 Dec;32(1):2545519. doi: 10.1080/10717544.2025.2545519. Epub 2025 Aug 17. Drug Deliv. 2025. PMID: 40819311 Free PMC article.
Efficient formulation of SN-38 for broad-spectrum chemotherapy remains an unmet medical need. The limited solubility of SN-38 in both aqueous and organic solvents poses a major challenge for formulation development. ...The major issue of SN-3 …
Efficient formulation of SN-38 for broad-spectrum chemotherapy remains an unmet medical need. The limited solubility of SN …
Investigation into the Efficacy of Val-SN-38, a Valine-Ester Prodrug of the Anti-Cancer Agent SN-38.
Kwak EY, Choi MK, Yang SG, Shim CK, Shim WS. Kwak EY, et al. Biomol Ther (Seoul). 2012 May;20(3):326-31. doi: 10.4062/biomolther.2012.20.3.326. Biomol Ther (Seoul). 2012. PMID: 24130931 Free PMC article.
As only the lactone form is known to have cytotoxic activity, the proportion of lactone in Val-SN-38 and SN-38 was determined, but no differences were found. However, it turned out that Val-SN-38 had poor stability compared …
As only the lactone form is known to have cytotoxic activity, the proportion of lactone in Val-SN-38 and SN …
Pharmacology of irinotecan.
Robert J, Rivory L. Robert J, et al. Drugs Today (Barc). 1998 Sep;34(9):777-803. doi: 10.1358/dot.1998.34.9.485276. Drugs Today (Barc). 1998. PMID: 14988754
The carboxylesterase which carries out this conversion is preferentially active on the lactone form of irinotecan and directly generates the lactone form of SN-38, which may explain the superiority of irinotecan over SN-38 i …
The carboxylesterase which carries out this conversion is preferentially active on the lactone form of irinotecan and directly …
287 results