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Irinotecan hydrochloride Sale

(Synonyms: 伊立替康盐酸盐; (+)-Irinotecan hydrochloride; CPT-11 hydrochloride) 目录号 : GC36329

A potent inhibitor of DNA topoisomerase I

Irinotecan hydrochloride Chemical Structure

Cas No.:100286-90-6

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产品描述

Irinotecan, a derivative of the alkaloid camptothecin , functions as a prodrug that is converted by tissue carboxylesterase to 7-ethyl-10-hydroxycamptothecin, a potent inhibitor of DNA topoisomerase I.1,2 Its action is terminated by glucuronidation by UDP glucuronosyl transferase 1A1.3,4 Irinotecan demonstrates a broad spectrum of antitumor activity against metastatic colorectal cancer, small cell lung cancer, and several other solid tumors and has proven useful in radiation treatment of tumors by sensitizing tissue to radiation damage.1,2

1.Rothenberg, M.L.Topoisomerase I inhibitors: Review and updateAnn. Oncol.8(9)837-855(1997) 2.Dancey, J., and Eisenhauer, E.A.Current perspectives on camptothecins in cancer treatmentBr. J. Cancer74(3)327-338(1996) 3.Mathijssen, R.H.J., van Alphen, R.J., Verweij, J., et al.Clinical pharmacokinetics and metabolism of irinotecan (CPT-11)Clin. Cancer Res.7(8)2182-2194(2001) 4.Ma, M.K., and McLeod, H.L.Lessons learned from the irinotecan metabolic pathwayCurr. Med. Chem.10(1)41-49(2003)

Chemical Properties

Cas No. 100286-90-6 SDF
别名 伊立替康盐酸盐; (+)-Irinotecan hydrochloride; CPT-11 hydrochloride
Canonical SMILES O=C(N1CCC(N2CCCCC2)CC1)OC3=CC=C4N=C5C(CN6C(C(COC([C@@]7(CC)O)=O)=C7C=C65)=O)=C(CC)C4=C3.[H]Cl
分子式 C33H39ClN4O6 分子量 623.14
溶解度 DMSO: ≥ 51 mg/mL (81.84 mM); Water: 3.33 mg/mL (5.34 mM) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.6048 mL 8.0239 mL 16.0478 mL
5 mM 0.321 mL 1.6048 mL 3.2096 mL
10 mM 0.1605 mL 0.8024 mL 1.6048 mL
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Research Update

Pegylated Liposomal Irinotecan hydrochloride Trihydrate for Treating Pancreatic Cancer After Gemcitabine: An Evidence Review Group Perspective of a NICE Single Technology Appraisal

Pharmacoeconomics 2018 Mar;36(3):289-299.PMID:29178025DOI:10.1007/s40273-017-0592-3.

The National Institute for Health and Care Excellence (NICE) invited the manufacturer (Shire Pharmaceuticals) of pegylated liposomal Irinotecan hydrochloride trihydrate (liposomal irinotecan) to submit clinical and cost-effectiveness evidence for its use in combination with 5-fluorouracil (5-FU) and folic acid/leucovorin (LV) for treating patients with pancreatic cancer following prior treatment with gemcitabine as part of the institute's Single Technology Appraisal process. The Liverpool Reviews and Implementation Group at the University of Liverpool was commissioned to act as the Evidence Review Group (ERG). This article presents a summary of the company's evidence, the ERG review and the resulting NICE guidance (TA440), issued on 26 April 2017. Clinical evidence for liposomal irinotecan + 5-FU/LV versus 5-FU/LV was derived from 236 patients with metastatic pancreatic cancer in the multinational, open-label, randomised controlled NAPOLI-1 trial. Results from analyses of progression-free survival and overall survival showed statistically significant improvements for patients treated with liposomal irinotecan + 5-FU/LV compared with those treated with 5-FU/LV. However, 5-FU/LV alone is rarely used in National Health Service clinical practice for patients with metastatic pancreatic cancer previously treated with gemcitabine. The company, ERG and Appraisal Committee (AC) all agreed that oxaliplatin + 5-FU/LV is the most commonly used treatment. Oxaliplatin + 5-FU/LV was compared with 5-FU/LV in two trials identified by the company. However, the company and the ERG both considered attempts to compare the efficacy of liposomal irinotecan + 5-FU/LV with oxaliplatin + 5-FU/LV to be methodologically flawed; not only was there heterogeneity between trials and their populations but also the proportional hazards assumption required to conduct a robust indirect treatment comparison (ITC) was violated. Nonetheless, data derived from an ITC were used to inform the company's economic model. Using the discounted patient access scheme price for liposomal irinotecan + 5-FU/LV, the company reported an incremental cost-effectiveness ratio (ICER) per quality-adjusted life-year (QALY) gained of £54,412 for the comparison with oxaliplatin + 5-FU/LV. The ERG considered that the company's base-case cost-effectiveness results for the comparison of liposomal irinotecan + 5-FU/LV versus oxaliplatin + 5-FU/LV were underestimates and should be interpreted with extreme caution. Following implementation of a number of model amendments, the ERG's modified exploratory ICER for the comparison of liposomal irinotecan + 5-FU/LV versus oxaliplatin + 5-FU/LV was £106,898 per QALY gained. The AC accepted the majority of the ERG's amendments to the model, and also highlighted that the total QALYs for oxaliplatin + 5-FU/LV were lower than for 5-FU/LV in the company's model, which the AC considered to be clinically implausible. The AC therefore considered results from exploratory analyses, undertaken by the ERG, which included altering the QALY difference between liposomal irinotecan + 5-FU/LV and oxaliplatin + 5-FU/LV by ± 10%. These analyses resulted in ICERs for the comparison of liposomal irinotecan + 5-FU/LV versus oxaliplatin + 5-FU/LV of between £201,019 per QALY gained to liposomal irinotecan + 5-FU/LV being dominated by oxaliplatin + 5-FU/LV. Therefore, despite uncertainty around the clinical-effectiveness evidence and cost-effectiveness results, the AC was confident that the ICER was in excess of £50,000 per QALY gained. The final guidance issued by NICE is that liposomal irinotecan + 5-FU/LV is not recommended within its marketing authorisation for treating metastatic adenocarcinoma of the pancreas in adults whose disease has progressed after gemcitabine-based therapy.

[Irinotecan hydrochloride (CPT-11)]

Gan To Kagaku Ryoho 1994 Apr;21(5):709-17.PMID:8154899doi

Irinotecan hydrochloride (CPT-11) is a water-soluble semisynthetic derivative of camptothecin. CPT-11 is a prodrug that undergoes deesterification in vivo to produce SN-38, a metabolite that is 1,000-fold more potent than the parent compound in vitro. CPT-11 is a potent topoisomerase I inhibitor with a broad spectrum of experimental antitumor activity. Recent clinical trials also reveal that CPT-11 is very effective in the treatment of cancers including lung cancer, cervix cancer, ovary cancer, etc. Now, comparative trials of combination chemotherapy in responsive tumors are indicated from these excellent clinical results.

Irinotecan plus cisplatin compared with etoposide plus cisplatin for extensive small-cell lung cancer

N Engl J Med 2002 Jan 10;346(2):85-91.PMID:11784874DOI:10.1056/NEJMoa003034.

Background: Irinotecan hydrochloride, a topoisomerase I inhibitor, is effective against small-cell lung cancer. In a phase 2 study of irinotecan plus cisplatin in patients with extensive small-cell lung cancer, there was a high response rate and a promising median survival time. Methods: We conducted a multicenter, randomized, phase 3 study in which we compared irinotecan plus cisplatin with etoposide plus cisplatin in patients with extensive (metastatic) small-cell lung cancer. Results: The planned size of the study population was 230 patients, but enrollment was terminated early because an interim analysis found a statistically significant difference in survival between the patients assigned to receive irinotecan and cisplatin and those assigned to receive etoposide and cisplatin; as a result, only 154 patients were enrolled. The median survival was 12.8 months in the irinotecan-plus-cisplatin group and 9.4 months in the etoposide-plus-cisplatin group (P=0.002 by the unadjusted log-rank test). At two years, the proportion of patients surviving was 19.5 percent in the irinotecan-plus-cisplatin group and 5.2 percent in the etoposide-plus-cisplatin group. Severe or life-threatening myelosuppression was more frequent in the etoposide-plus-cisplatin group than in the irinotecan-plus-cisplatin group, and severe or life-threatening diarrhea was more frequent in the irinotecan-plus-cisplatin group than in the etoposide-plus-cisplatin group. Conclusions: Irinotecan plus cisplatin is an effective treatment for metastatic small-cell lung cancer.

Irinotecan hydrochloride: drug profile and nursing implications of a topoisomerase I inhibitor in patients with advanced colorectal cancer

Oncol Nurs Forum 1998 Apr;25(3):535-43.PMID:9568608doi

Purpose/objectives: To review the drug profile and nursing implications of the topoisomerase I inhibitor Irinotecan hydrochloride. Data sources: Published articles, abstracts, professional communications, drug manufacturer, and professional clinical experience with irinotecan clinical studies. Data synthesis: Irinotecan, one of the first topoisomerase I inhibitors to gain wide clinical use, has exhibited activity in several malignancies. In June 1996, the United States Food and Drug Administration approved its use in patients with metastatic colorectal cancer refractory to fluorouracil (5-FU)-based therapy. The recommended starting dose is 125 mg/m2 administered as a weekly infusion for four weeks followed by a two-week rest period. The most common and clinically significant adverse events include diarrhea, neutropenia, and nausea and vomiting. Other adverse events include alopecia and fatigue. Conclusions: Irinotecan has significant activity in patients with 5-FU-refractory colorectal cancer. This drug is well tolerated and easily administered in an outpatient setting. The most common adverse events are well characterized and are reversible upon treatment discontinuation or dosage reduction. In particular, diarrhea, the most common toxicity, is manageable with use of appropriate dose modification and rigorous administration of loperamide at the first signs of diarrhea. Implications for nursing practice: Nurses need to focus on identifying and managing adverse effects based on individual patient tolerance. Nurses have an important role to play in patient education and follow up in order to minimize toxicity. Patient care concerns include management of diarrhea and nausea and vomiting, neutropenia with related risk of infection, and fluid and electrolyte imbalances.

Clinical trials of Irinotecan hydrochloride (CPT, campto injection, topotecin injection) in Japan

Ann N Y Acad Sci 1996 Dec 13;803:292-305.PMID:8993523DOI:10.1111/j.1749-6632.1996.tb26399.x.

CPT-11 was synthesized in 1984 at the laboratory of Yakult Honsha. Phase I study of CPT-11 was begun in 1986. The appropriate doses for phase II studies were decided to be 100 mg/m2 weekly or 150 mg/m2 every 2 weeks. Phase II study was conducted and this drug was approved for NSCLC, SCLC, uterine cancer and ovarian cancer by MHW in 1994. It obtained approval for stomach cancer, colorectal cancer, breast cancer, skin cancer and non-Hodgkin's lymphoma in 1995. The combination chemotherapies including CPT-11 have been conducted by using various regimens such as CPT-11 + CDDP, CPT-11 + VP-16, CPT-11 + 5-FU and CBDCA + CPT-11. In stage IV SCLC two prospective randomized controlled trials are on going comparing CPT-11 vs. CPT-11 + CDDP vs. VDS + CDDP and CPT-11 + CDDP vs. VDS + CDDP. In advanced SCLC Japanese Clinical Oncology Group (JCOG) started a randomized controlled trial comparing CPT-11 + CDDP vs. VP-16 + CDDP. In stage III NSCLC the dose escalation studies of CPT-11 (CPT-11) in the combination with TRT are ongoing by JCOG. The problem of CPT-11 in the combination chemotherapy and combined modality is that it is quite difficult to increase the dose of CPT-11 to full dose to obtain the maximum effect.