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  • topotecan
  • Both cell lines were 400- to 1000-fold more resistant to topotecan, 9-amino-20( S )-camptothecin, and the active metabolite of irinotecan, 7-ethyl-10-hydroxycamptothecin (SN-38), than their parental cell lines. (aacrjournals.org)
  • The discovery of Camptothecin spurred the development of many derivatives with superior activity and solubility, including Irinotecan (sc-202186) and Topotecan (sc-204919). (protocol-online.org)
  • Over the past decade, camptothecin agents such as topotecan and irinotecan have demonstrated activity against Ewing sarcoma, especially in combination with alkylating agents. (hindawi.com)
  • Modulation of the camptothecin topotecan, approved for second-line therapy, may improve response. (mdpi.com)
  • I. To evaluate the effect of second-line treatment with CRLX101 (cyclodextrin-based polymer-camptothecin CRLX101) compared to intravenous (IV) topotecan hydrochloride (topotecan) on progression free survival (PFS) of patients with extensive-stage small cell lung cancer (ES-SCLC) sensitive to first-line platinum-based chemotherapy. (knowcancer.com)
  • Depletion of glutathione (GSH) in MCF-7 and MDA-MB-231 cell lines by pretreatment with the GSH synthesis inhibitor buthionine sulfoximine potentiated the activity of 10,11-methylenedioxy-20(S)-camptothecin, SN-38 [7-ethyl-10-hydroxy-20(S)-camptothecin], topotecan, and 7-chloromethyl-10,11-methylenedioxy-20(S)camptothecin (CMMDC). (rti.org)
  • sublines
  • We studied resistance to the camptothecins in two sublines expressing high levels of MXR: S1-M1-80 cells derived from parental S1 colon cancer cells and MCF-7 AdVp3000 isolated from parental MCF-7 breast cancer cells. (aacrjournals.org)
  • phase I clin
  • Camptothecin (CPT) has recently been undergoing phase I clinical trials. (protocol-online.org)
  • 9-Amino-20( S )-camptothecin (9-AC) has demonstrated efficacy against several human cancer xenografts, including cancers of the colon, breast, lung, ovary, and stomach and malignant melanoma, and is currently undergoing Phase I clinical trials. (aacrjournals.org)
  • Apoptosis
  • Anne Cox, Dawn A. Bradbury, Tracy D. Simmons, Kevin J. Slater, and Sharon P. M. Crouch, "Determination of the Effects of Camptothecin on Cell Cycling and Apoptosis in Human Leukaemic Cell Lines," TheScientificWorldJOURNAL , vol. 1, pp. 105-105, 2001. (hindawi.com)
  • chemotherapeutic
  • The camptothecin analog CPT-11 has recently been approved for the treatment of 5-fluorouracil (5-FU)-resistant colorectal cancer (1) , thus opening a new chapter in chemotherapeutic radiation sensitization. (springer.com)
  • resistance
  • The lack of selection for higher levels of UGT capacity in the colon cells suggests that high levels of expression of MXR alone are sufficient to confer resistance to the camptothecins. (aacrjournals.org)
  • Resistance to the camptothecins has been explored in model systems, and several putative mechanisms have been identified. (aacrjournals.org)
  • 1999 Camptothecin resistance: role of the ATP-binding cassette (ABC), mitoxantrone-resistance half-transporter (MXR), and potential for glucuronidation in MXR-expressing cells. (springer.com)
  • activity
  • Camptothecin was originally isolated from the stem wood of the Camptotheca acuminata tree and was shown to exhibit antileukemic/antitumour activity, and reversibly inhibit Mitochondrial Topo I (nuclear Topo I (topoisomerase I)) by binding to and stabilizing the topoisomerase-DNA covalent complex. (protocol-online.org)
  • All three derivatives [7-(gamma-glutamylcysteinylmethyl)-10,11-methylenedioxy-20(S)- camptothecin, 7-(cysteinylglycylmethyl)-10,11-methylenedioxy-20(S)-camptothecin, and 7-(cysteinylmethyl)-10,11-methylenedioxy-20(S)- camptothecin] displayed topo I and, cell growth-inhibitory activity. (rti.org)
  • human
  • Mutations in Cullin 4B result in a human syndrome associated with increased camptothecin-induced topoisomerase I-dependent DNA breaks. (nih.gov)
  • The parent camptothecin molecule is compromised in its clinical utility by several factors: it is poorly water soluble ( 2 ), and it undergoes conversion at physiologic pH to the inactive carboxylate form ( 3 ) of the drug, which binds avidly to human serum albumin ( 3 - 5 ). (aacrjournals.org)
  • respectively
  • The pharmacokinetic profile of conjugated and unconjugated camptothecin showed a polyexponential decline with similar terminal half life ( t 1/2 range was 44-63 and 31-48 h for conjugated and unconjugated, respectively). (aacrjournals.org)
  • Urinary excretion of conjugated and unconjugated camptothecin accounted for about 30% and 4% of the administered dose, respectively. (aacrjournals.org)