Amrubicin - CAS 110267-81-7
Catalog number: 110267-81-7
Category: Inhibitor
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Molecular Formula:
C25H25NO9
Molecular Weight:
483.47
COA:
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Targets:
Others
Description:
Amrubicin is a novel anthracycline derivative for treatment of bladder carcinoma.
Purity:
>98%
Synonyms:
SM-5887
MSDS:
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InChIKey:
VJZITPJGSQKZMX-XDPRQOKASA-N
InChI:
InChI=1S/C25H25NO9/c1-10(27)25(26)7-13-18(16(8-25)35-17-6-14(28)15(29)9-34-17)24(33)20-19(23(13)32)21(30)11-4-2-3-5-12(11)22(20)31/h2-5,14-17,28-29,32-33H,6-9,26H2,1H3/t14-,15+,16-,17-,25-/m0/s1
Canonical SMILES:
CC(=O)C1(CC(C2=C(C3=C(C(=C2C1)O)C(=O)C4=CC=CC=C4C3=O)O)OC5CC(C(CO5)O)O)N
1.Pharmacokinetic and pharmacodynamic study on amrubicin and amrubicinol in Japanese patients with lung cancer.
Makino Y;Yamamoto N;Sato H;Ando R;Goto Y;Tanai C;Asahina H;Nokihara H;Sekine I;Kunitoh H;Ohe Y;Sugiyama E;Yokote N;Tamura T;Yamamoto H Cancer Chemother Pharmacol. 2012 Apr;69(4):861-9. doi: 10.1007/s00280-011-1768-8. Epub 2011 Nov 1.
PURPOSE: ;The pharmacokinetic (PK)-pharmacodynamic (PD) relationship of amrubicin and its active metabolite, amrubicinol, has only been evaluated using trough levels of these agents since the full PK profiles not yet been clarified so far. This study was performed to analyze the full PK profiles of amrubicin and amrubicinol and to evaluate their toxicity-PK relationships in Japanese patients.;METHODS: ;Amrubicin (35-40 mg/m(2)) was administered to 21 lung cancer patients on days 1-3 every 3-4 weeks. Fourteen blood samples were obtained per patient over the course of 3 administration days. The plasma concentrations of amrubicin and amrubicinol were quantitated by HPLC, and the relationships between PK parameters of these compounds and hematological toxicities were evaluated.;RESULTS: ;The overall PK profiles of amrubicin and amrubicinol were well characterized using a 3-compartment model and a 1-compartment model with a first-order metabolic process, respectively. The major toxicities were hematological. The clearance of amrubicinol was significantly correlated with grade 4 neutropenia (P = 0.01). The percentage decreases in the neutrophil count, hemoglobin level and platelet count were well correlated with the amrubicinol AUC.
2.[Second-line treatment and targeted therapy of advanced lung cancer].
Nakamura Y;Yamamoto N Gan To Kagaku Ryoho. 2009 May;36(5):710-6.
About ten years ago, docetaxel was established as a second-line chemotherapy for advanced non-small cell lung cancer(NSCLC). After that, pemetrexed has been shown to be similar to docetaxel in response rate, overall survival and progression-free survival, and to have a more favorable toxicity profile. As a result, pemetrexed was approved in the US and Europe. On the other hand, EGFR TKI has been compared to docetaxel or best supportive care in phase III trials. Based on these results, EGFR-TKI is now considered one of the treatment options in a second-line setting for NSCLC. Recently, it has been shown that EGFR-TKIs are very effective against EGFR mutation-positive NSCLC in many reports. Thus, EGFR-TKIs are examined as first-line chemotherapy against those patients. Since, other molecular- targeted drugs except for EGFR-TKI have been developed, we hope for the establishment of further effective second- line treatment for NSCLC. As for small cell lung cancer, phase III trials for second-line treatment are few. Topotecan is the only agent which has been proved to show a significant prolongation of survival for the best supportive care. In Japan, amrubicin is considered an effective agent for relapsed small cell lung cancer.
3.Amrubicin for relapsed small-cell lung cancer: a systematic review and meta-analysis of 803 patients.
Horita N;Yamamoto M;Sato T;Tsukahara T;Nagakura H;Tashiro K;Shibata Y;Watanabe H;Nagai K;Nakashima K;Ushio R;Ikeda M;Kobayashi N;Shinkai M;Kudo M;Kaneko T Sci Rep. 2016 Jan 11;6:18999. doi: 10.1038/srep18999.
Currently, amrubicin is permitted for relapsed small-cell lung carcinoma (SCLC) only in Japan. The efficacy and adverse effects of amrubicin as reported by previous studies varied greatly. The inclusion criterion was a prospective study that was able to provide data for efficacy and safety by the AMR single agent regimen as second-line chemotherapy for a patient with SCLC. Binary data were meta-analyzed with the random-model generic inverse variance method. We included nine articles consisted of 803 patients. The pooled three-, six-, and nine-month progression-free survival were 63% (95% CI 57-69%, I(2) = 53%), 28% (95% CI 21-35%, I(2) = 71%), and 10% (95% CI 6-14%, I(2) = 41%), respectively. The pooled six-, 12-, and 18-month overall survival were 69% (95% CI 61-78%, I(2) = 83%), 36% (95% CI 28-44%, I(2) = 80%), and 15% (95% CI 8-21%, I(2) = 81%), respectively. Amrubicin seemed much more beneficial for Japanese patients. However, compared to the efficacy of topotecan presented in a previous meta-analysis, amrubicin may be a better treatment option than topotecan for both Japanese and Euro-American. Adverse effects by amrubicin were almost exclusively observed to be hematological. Notably, grade III/IV neutropenia incidence was 70% and febrile neutropenia incidence was 12%.
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CAS 110267-81-7 Amrubicin

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