amrubicin profile

amrubicin: structure in first source; a 9-amino-anthracycline antibiotic [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

amrubicin : A synthetic anthracycline antibiotic with molecular formula C25H25NO9. A specific inhibitor of topoisomerase II, it is used (particularly as the hydrochloride salt) in the treatment of cancer, especially lung cancer, where it is a prodrug for the active metabolite, ambrucinol. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	3035016
CHEMBL ID	1186894
CHEBI ID	135779
SCHEMBL ID	9140
MeSH ID	M0300373

Synonym
amrubicin
amrubicin [inn]
(+-)-(7s,9s)-9-acetyl-9-amino-7-((2-deoxy-beta-d-erythro-pentopyranosyl)oxy)-7,8,9,10-tetrahydro-6,11-dihydroxy-5,12-naphthacenedione
CHEBI:135779
amrubicinum
amrubicine
amrubicina
(1s,3s)-3-acetyl-3-amino-5,12-dihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 2-deoxy-beta-d-erythro-pentopyranoside
(7s,9s)-9-acetyl-9-amino-7-{[(2s,4s,5r)-4,5-dihydroxytetrahydro-2h-pyran-2-yl]oxy}-6,11-dihydroxy-7,8,9,10-tetrahydrotetracene-5,12-dione
D08854
amrubicin (usan/inn)
110267-81-7
(7s,9s)-9-acetyl-9-amino-7-[(2s,4s,5r)-4,5-dihydroxyoxan-2-yl]oxy-6,11-dihydroxy-8,10-dihydro-7h-tetracene-5,12-dione
unii-93n13lb4z2
5,12-naphthacenedione, 9-acetyl-9-amino-7-((2-deoxy-beta-d-erythro-pentopyranosyl)oxy)-7,8,9,10-tetrahydro-6,11-dihydroxy-, (7s,9s)-
93n13lb4z2 ,
amrubicin [usan:inn]
W-60403
CHEMBL1186894
HY-B0067
SCHEMBL9140
amrubicin [usan]
amrubicin [mart.]
amrubicin [who-dd]
amrubicin [mi]
VJZITPJGSQKZMX-XDPRQOKASA-N
W-200813
AC-31129
EX-A161
AKOS030526071
(7s,9s)-9-acetyl-9-amino-7-(((2s,4s,5r)-4,5-dihydroxytetrahydro-2h-pyran-2-yl)oxy)-6,11-dihydroxy-7,8,9,10-tetrahydrotetracene-5,12-dione
amrubicin(sm-5887)
(+)-(7s,9s)-9-acetyl-9-amino-7-[(2-deoxy--d-erythro-pentopyranosyl)oxy]-7,8,9,10-tetrahydro-6,11-dihydroxy-5,12-naphthacenedione hydrochloride
DB06263
Q4748723

Excerpt	Reference	Relevance
"Amrubicin chemotherapy is a treatment option for patients with non-small cell lung cancer (NSCLC) after third-line treatment in Japan. "	( Clinical significance of topoisomerase-II expression in patients with advanced non-small cell lung cancer treated with amrubicin. Hisada, T; Kaira, K; Miura, Y; Oyama, T; Saito, R; Sakurai, R; Sunaga, N; Yamada, M, 2020)	2.21
"Amrubicin (AMR) is a next-generation anthracycline that is commonly used to treat lung cancer."	( Premature phase II study of amrubicin as palliative chemotherapy for previously treated malignant pleural mesothelioma. Hosomi, Y; Kawai, S; Nagamata, M; Okuma, Y; Watanabe, K, 2021)	1.64
"Amrubicin monotherapy is a treatment option for patients with relapsed small cell lung cancers (SCLCs). "	( High expression of topoisomerase-II predicts favorable clinical outcomes in patients with relapsed small cell lung cancers receiving amrubicin. Hisada, T; Kaira, K; Miura, Y; Saito, R; Sakurai, R; Sunaga, N; Yamada, M, 2018)	2.13
"Amrubicin is a synthetic anthracycline with single-agent activity in relapsed/refractory SCLC."	( Amrubicin and carboplatin with pegfilgrastim in patients with extensive stage small cell lung cancer: A phase II trial of the Sarah Cannon Oncology Research Consortium. Burris, HA; Daniel, DB; Greco, FA; Hainsworth, JD; Mekhail, TM; Shipley, DL; Spigel, DR; Waterhouse, DM; Zubkus, JD, 2018)	2.64
"Amrubicin is a promising therapy for lung cancer, but is associated with a high incidence of severe neutropenia. "	( ABCB1 polymorphism as a predictive biomarker for amrubicin-induced neutropenia. Hijikata, H; Kawaguchi, Y; Kunii, E; Maeno, K; Nakao, M; Niimi, A; Oguri, T; Ohkubo, H; Takakuwa, O; Takemura, M; Uemura, T, 2014)	2.1
"Amrubicin is a synthetic anthracycline which has been shown in preclinical studies to have broad-spectrum anti-tumor activity and a lower potential for cardiotoxicity as compared to doxorubicin. "	( Amrubicin as second- or third-line treatment for women with metastatic HER2-negative breast cancer: a Sarah Cannon Research Institute phase 1/2 trial. Burris, HA; Hainsworth, JD; Inclan, A; Priego, V; Raefsky, E; Yardley, DA, 2014)	3.29
"Amrubicin appears to be a promising agent for relapsed SCLC, but its effectiveness in CNS metastases originating from SCLC is unknown."	( The efficacy of amrubicin on central nervous system metastases originating from small-cell lung cancer: a case series of eight patients. Akamatsu, H; Endo, M; Kaira, K; Kaira, R; Kenmotsu, H; Miura, S; Murakami, H; Naito, T; Nakamura, Y; Ono, A; Shukuya, T; Takahashi, T; Tsuya, A; Yamamoto, N, 2015)	1.48
"Amrubicin is a third generation synthetic 9-aminoanthracycline that specifically inhibits topoisomerase II. "	( Phase II study of amrubicin (SM-5887), a synthetic 9-aminoanthracycline, as first line treatment in patients with metastatic or unresectable soft tissue sarcoma: durable response in myxoid liposarcoma with TLS-CHOP translocation. Boucher, K; Chawla, S; Gouw, L; Gupta, S; Pitt, D; Sharma, S; Wade, M; Wright, J, 2016)	2.21
"Amrubicin is a totally synthetic anthracycline anticancer drug that acts as a potent topoisomerase II inhibitor."	( Amrubicin for the treatment of advanced lung cancer. Kurata, T, 2009)	2.52
"Amrubicinol (AMR-OH) is an active metabolite of amrubicin (AMR), a novel synthetic 9-aminoanthracycline derivative. "	( Plasma concentration of amrubicinol in plateau phase in patients treated for 3 days with amrubicin is correlated with hematological toxicities. Asai, K; Hirata, K; Kimura, T; Kudoh, S; Kyoh, S; Mitsuoka, S; Tanaka, H; Tochino, Y; Umekawa, K; Yoshimura, N, 2009)	2.1
"Amrubicin is a synthetic anthracyclin analogue that has significant activity in Japanese patients with extensive stage small cell lung cancer (ES-SCLC). "	( Amrubicin: a synthetic anthracyclin analogue in the treatment of extensive stage small cell lung cancer. Shah, CM, 2009)	3.24
"Amrubicin is a new anticancer drug that has been shown to exert efficacy against small cell lung cancer. "	( [Pharmacokinetic study of amrubicin in a case of small lung cancer on hemodialysis]. Chihara, S; Demizu, M; Hosoi, K; Igarashi, T; Min, K; Nakashima, Y; Ohsawa, M; Tomiyama, N; Ueda, H, 2009)	2.1
"Amrubicin is an active and well-tolerated regimen in patients with previously treated lung cancer. "	( A phase II study of amrubicin, a synthetic 9-aminoanthracycline, in patients with previously treated lung cancer. Fueki, N; Hisada, T; Iijima, H; Imai, H; Ishizuka, T; Iwasaki, Y; Kaira, K; Mori, M; Saito, R; Shimizu, K; Sunaga, N; Tomizawa, Y; Tsurumaki, H; Utsugi, M; Yanagitani, N; Yoshii, A, 2010)	2.13
"Amrubicin is a synthetic anthracycline drug that is a potent inhibitor of topoisomerase II. "	( Phase II trial of amrubicin for second-line treatment of advanced non-small cell lung cancer: results of the West Japan Thoracic Oncology Group trial (WJTOG0401). Akita, K; Fukuoka, M; Goto, I; Hayashi, H; Iwamoto, Y; Kaneda, H; Kimura, T; Kudoh, S; Miyazaki, M; Nakagawa, K; Okamoto, I; Saito, H; Satouchi, M; Sawa, T; Shibata, K; Sugiura, T; Takeda, K; Yoshioka, H, 2010)	2.14
"Amrubicin is a possible alternative for second-line treatment of advanced NSCLC, although a relevant hematological toxicity is significant, especially with a febrile neutropenia."	( Phase II trial of amrubicin for second-line treatment of advanced non-small cell lung cancer: results of the West Japan Thoracic Oncology Group trial (WJTOG0401). Akita, K; Fukuoka, M; Goto, I; Hayashi, H; Iwamoto, Y; Kaneda, H; Kimura, T; Kudoh, S; Miyazaki, M; Nakagawa, K; Okamoto, I; Saito, H; Satouchi, M; Sawa, T; Shibata, K; Sugiura, T; Takeda, K; Yoshioka, H, 2010)	2.14
"Amrubicin is a synthetic anthracycline with potent topoisomerase II inhibition. "	( Phase II study of amrubicin as second-line therapy in patients with platinum-refractory small-cell lung cancer. Alemany, C; Conkling, P; Dudek, AZ; Ettinger, DS; Garbo, L; Gupta, V; Jotte, R; Lorigan, P; McNally, R; Oliver, JW; Renschler, MF; Salgia, R; Shah, C; Spigel, DR, 2010)	2.14
"Amrubicin is a novel anthracycline agent that is well known to exert significant activity against small cell lung cancer (SCLC), but the adverse pulmonary effects of amrubicin are less well known. "	( Severe interstitial lung disease associated with amrubicin treatment. Goto, K; Kenmotsu, H; Kubota, K; Niho, S; Nishiwaki, Y; Ohe, Y; Ohmatsu, H; Saijo, N; Yamaguchi, Y; Yoh, K, 2010)	2.06
"Amrubicin is a novel, totally synthesized anthracycline derivative, and has antitumor activity against several human tumor xenografts. "	( Phase II trial of amrubicin and carboplatin in patients with sensitive or refractory relapsed small-cell lung cancer. Adachi, M; Hirose, T; Kusumoto, S; Nakashima, M; Ohmori, T; Ohnishi, T; Okuda, K; Shirai, T; Sugiyama, T; Yamaoka, T, 2011)	2.15
"Amrubicin (AMR) is an active agent for relapsed small cell lung cancer (SCLC). "	( Clinical outcome of amrubicin therapy according to the prior chemotherapy sensitivities of extensive small cell lung cancer. Hirata, K; Kimura, T; Kudoh, S; Mitsuoka, S; Nagata, M; Suzumura, T; Tanaka, H; Ueda, T; Umekawa, K; Yoshimura, N, 2011)	2.14
"Amrubicin is an active agent for the treatment of small-cell lung cancer (SCLC). "	( Long-term amrubicin chemotherapy for small-cell lung cancer. Goya, S; Higashiguchi, M; Hirashima, T; Kawase, I; Kobayashi, M; Matsuura, Y; Morishita, N; Okamoto, N; Suzuki, H; Tamiya, M, 2012)	2.22
"Amrubicin (AMR) is a novel, completely synthetic 9-aminoanthracycline derivative. "	( Additive effects of amrubicin with cisplatin on human lung cancer cell lines. Hirata, K; Kimura, T; Kudoh, S; Yamauchi, S; Yoshikawa, J, 2002)	2.08
"Amrubicin is a completely synthetic anthracycline derivative. "	( [Profile of the anti-tumor effects of amrubicin, a completely synthetic anthracycline]. Hanada, M; Murayama, T; Noguchi, T, 2003)	2.03
"Amrubicin is a novel, totally synthetic 9-aminoanthracycline. "	( Phase I/II study of amrubicin, a novel 9-aminoanthracycline, in patients with advanced non-small-cell lung cancer. Ariyoshi, Y; Fukuoka, M; Ikegami, H; Nakamura, S; Negoro, S; Sugiura, T; Takada, M; Yana, T, 2005)	2.09
"Amrubicin is a novel synthetic 9-aminoanthracycline derivative and is converted enzymatically to its C-13 hydroxy metabolite, amrubicinol, whose cytotoxic activity is 10-100 times that of amrubicin. "	( Phase I and pharmacokinetic study of amrubicin, a synthetic 9-aminoanthracycline, in patients with refractory or relapsed lung cancer. Fujii, S; Hamada, A; Kishi, H; Matsunaga, Y; Mori, I; Okamoto, I; Saito, H; Sasaki, J; Semba, H; Uramoto, H; Yamagata, H, 2006)	2.05
"Amrubicin is a novel 9-aminoanthracycline. "	( Multicenter phase II study of amrubicin, 9-amino-anthracycline, in patients with advanced non-small-cell lung cancer (Study 1): West Japan Thoracic Oncology Group (WJTOG) trial. Ariyoshi, Y; Isobe, T; Kamei, T; Katakami, N; Kawakami, A; Kudoh, S; Nakanishi, Y; Sawa, T; Sugiura, T; Takada, M; Tohda, Y; Yamamoto, H; Yana, T; Yokota, S, 2006)	2.07
"Amrubicin is a synthetic 9-aminoanthracycline that has significant antitumor activity in Japanese patients with extensive stage small cell lung cancer (SCLC). "	( Amrubicin for the treatment of small cell lung cancer: does effectiveness cross the Pacific? Ettinger, DS, 2007)	3.23
"Amrubicin is a totally synthetic anthracycline anticancer drug and a potent topoisomerase II inhibitor. "	( Amrubicin for non-small-cell lung cancer and small-cell lung cancer. Fukuoka, M; Kurata, T; Okamoto, I; Tamura, K, 2007)	3.23
"Amrubicin is a completely synthetic 9-aminoanthracycline agent for the treatment of lung cancer in Japan. "	( Role of P-glycoprotein in accumulation and cytotoxicity of amrubicin and amrubicinol in MDR1 gene-transfected LLC-PK1 cells and human A549 lung adenocarcinoma cells. Fujii, J; Hamada, A; Hira, A; Maeda, Y; Saito, H; Sanematsu, E; Sasaki, J; Watanabe, H; Yokoo, K, 2008)	2.03
"Amrubicin is a novel, completely synthetic 9-aminoanthracycline derivative. "	( A new antitumor agent amrubicin induces cell growth inhibition by stabilizing topoisomerase II-DNA complex. Fukushima, A; Hanada, M; Mizuno, S; Noguchi, T; Saito, Y; Yamaoka, T, 1998)	2.06

Excerpt	Reference	Relevance
"Amrubicinol has a higher activity level inside the cells than does amrubicin."	( Cytotoxicity of amrubicin, a novel 9-aminoanthracycline, and its active metabolite amrubicinol on human tumor cells. Hanada, M; Ichii, S; Morisada, S; Noguchi, T; Yamaoka, T; Yanagi, Y, 1998)	1.37
"Amrubicin (AMR) has become the standard of care for post-relapse small cell lung cancer (SCLC). "	( Influencing factors of efficacy and long-term use of amrubicin in patients with small cell lung cancer. Ishige, Y; Kato, R; Mizuno, S; Nakase, K; Nishiki, K; Nojiri, M; Oikawa, T; Sakuma, T; Shinomiya, S; Shionoya, I; Takahara, Y; Tanaka, T; Yamamura, K, 2023)	2.6
"Amrubicin (AMR) has shown promising activity for lung cancer. "	( Amphiregulin as a Novel Resistance Factor for Amrubicin in Lung Cancer Cells. Kamiryo, H; Katsurada, M; Kobayashi, K; Nagano, T; Nakata, K; Nishimura, Y; Tachihara, M; Tokunaga, S; Yamamoto, M; Yokozaki, H, 2017)	2.16
"Amrubicin has efficacy comparable to doxorubicin in adult STS, is well tolerated and has no significant cardiac toxicity up to a cumulative dose of 4800 mg /m(2). "	( Phase II study of amrubicin (SM-5887), a synthetic 9-aminoanthracycline, as first line treatment in patients with metastatic or unresectable soft tissue sarcoma: durable response in myxoid liposarcoma with TLS-CHOP translocation. Boucher, K; Chawla, S; Gouw, L; Gupta, S; Pitt, D; Sharma, S; Wade, M; Wright, J, 2016)	2.21
"Amrubicin has demonstrated single-agent activity in multiple phase II trials in both chemotherapy-sensitive and -refractory relapse."	( Management of small-cell lung cancer: incremental changes but hope for the future. Hann, CL; Rudin, CM, 2008)	1.07
"Amrubicinol has a higher activity level inside the cells than does amrubicin."	( Cytotoxicity of amrubicin, a novel 9-aminoanthracycline, and its active metabolite amrubicinol on human tumor cells. Hanada, M; Ichii, S; Morisada, S; Noguchi, T; Yamaoka, T; Yanagi, Y, 1998)	1.37

Excerpt	Reference	Relevance
"Amrubicin treatment resulted in a significantly higher ORR than topotecan (44% v 15%; P = .021)."	( Randomized phase II trial of single-agent amrubicin or topotecan as second-line treatment in patients with small-cell lung cancer sensitive to first-line platinum-based chemotherapy. Conkling, P; Fitzgibbons, JF; Galsky, MD; Jotte, R; Klein, L; McNally, R; Oliver, JW; Renschler, MF; Reynolds, C, 2011)	1.35
"Treatment with amrubicin appeared effective in SCLC patients previously treated with chemotherapy, although it was not necessarily safe, because of myelosuppression. "	( Retrospective analysis of efficacy and safety of amrubicin in refractory and relapsed small-cell lung cancer. Gemma, A; Hibino, S; Hosomi, Y; Iguchi, M; Kitamura, K; Okamura, T; Ota, T; Shibuya, M; Shimokawa, T, 2009)	0.96

Excerpt	Reference	Relevance
"Although amrubicin hydrochloride (AMR) has promising activity against pretreated lung cancer, there are few reports on the adverse events of this agent in a clinical practice setting."	( [Analysis of adverse events of amrubicin hydrochloride for pretreated lung cancer patients]. Maeda, R; Maruoka, H; Shibata, K; Takase, M, 2007)	1.04
" We have characterized how amrubicin converted to ROS or secondary alcohol metabolite in comparison with doxorubicin (that formed both toxic species) or epirubicin (that lacked ROS formation and showed an impaired conversion to alcohol metabolite)."	( Pharmacokinetic characterization of amrubicin cardiac safety in an ex vivo human myocardial strip model. II. Amrubicin shows metabolic advantages over doxorubicin and epirubicin. Aukerman, SL; Chello, M; Covino, E; Gonzalez Paz, O; Menna, P; Minotti, G; Salvatorelli, E; Sung, V; Surapaneni, S, 2012)	0.95
" Outcomes included progression-free survival (PFS), overall survival (OS), overall response rate (ORR), and adverse events."	( Efficacy and safety of amrubicin-based regimen used as first-line for extensive-disease small-cell lung cancer: A meta-analysis of randomized controlled trials. Cui, Y; Li, HW; Liao, F; Liu, CQ; Meng, XP; Tian, D; Wang, N; Yang, JD; Zhao, N; Zhao, S, 2018)	0.79
" The incidence of grade ≥3 adverse events was comparable between amrubicin-containing and other treatment groups (RR = 1."	( Efficacy and safety of amrubicin-based regimen used as first-line for extensive-disease small-cell lung cancer: A meta-analysis of randomized controlled trials. Cui, Y; Li, HW; Liao, F; Liu, CQ; Meng, XP; Tian, D; Wang, N; Yang, JD; Zhao, N; Zhao, S, 2018)	1.03
" Grade ≥ 3 hematological adverse events occurred as follows: decreased white blood cells in 52."	( Efficacy and safety of amrubicin monotherapy after atezolizumab plus carboplatin and etoposide in patients with relapsed small-cell lung cancer. Imai, H; Kagamu, H; Kaira, K; Kanazawa, K; Kishikawa, T; Minato, K; Minemura, H; Mouri, A; Nagai, Y; Shiihara, J; Shiono, A; Taniguchi, H; Tsuda, T; Wasamoto, S; Yamada, Y; Yamaguchi, O, 2022)	1.03

Excerpt	Reference	Relevance
" The method was successfully applied to a clinical pharmacokinetic study of amrubicin and amrubicinol in cancer patients."	( Simple and sensitive HPLC method for determination of amrubicin and amrubicinol in human plasma: application to a clinical pharmacokinetic study. Ando, R; Kimura, T; Makino, Y; Nishigaki, R; Tamura, T; Yamamoto, H; Yamamoto, N; Yokote, N, 2010)	0.84
" The pharmacokinetic parameters of amrubicin have not yet been investigated in hemodialysis patients, although it had been expected that amrubicin might not be cleared by hemodialysis because of its high lipid solubility, high protein binding rate and low urinary excretion rate."	( [Pharmacokinetic study of amrubicin in a case of small lung cancer on hemodialysis]. Chihara, S; Demizu, M; Hosoi, K; Igarashi, T; Min, K; Nakashima, Y; Ohsawa, M; Tomiyama, N; Ueda, H, 2009)	0.93
"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."	( Pharmacokinetic and pharmacodynamic study on amrubicin and amrubicinol in Japanese patients with lung cancer. Ando, R; Asahina, H; Goto, Y; Kunitoh, H; Makino, Y; Nokihara, H; Ohe, Y; Sato, H; Sekine, I; Sugiyama, E; Tamura, T; Tanai, C; Yamamoto, H; Yamamoto, N; Yokote, N, 2012)	0.88
"The pharmacokinetic profiles of amrubicin and amrubicinol were clarified, and the subsequent PK-PD analyses indicate that the clearance of amrubicinol is the major determinant of neutropenia."	( Pharmacokinetic and pharmacodynamic study on amrubicin and amrubicinol in Japanese patients with lung cancer. Ando, R; Asahina, H; Goto, Y; Kunitoh, H; Makino, Y; Nokihara, H; Ohe, Y; Sato, H; Sekine, I; Sugiyama, E; Tamura, T; Tanai, C; Yamamoto, H; Yamamoto, N; Yokote, N, 2012)	0.92
"Limited sampling points for both amrubicin (AMR) and its active metabolite amrubicinol (AMR-OH) were simultaneously optimized using Akaike's information criterion (AIC) calculated by pharmacokinetic modeling."	( Simultaneous optimization of limited sampling points for pharmacokinetic analysis of amrubicin and amrubicinol in cancer patients. Hayashi, Y; Makihara, RA; Makino, Y; Nokihara, H; Ohe, Y; Sato, H; Sugiyama, E; Watanabe, M; Yamamoto, N, 2016)	0.94
"In this pharmacokinetic study, 40 mg/m(2) of AMR was administered as a 5-min infusion on three consecutive days to 21 Japanese lung cancer patients."	( Simultaneous optimization of limited sampling points for pharmacokinetic analysis of amrubicin and amrubicinol in cancer patients. Hayashi, Y; Makihara, RA; Makino, Y; Nokihara, H; Ohe, Y; Sato, H; Sugiyama, E; Watanabe, M; Yamamoto, N, 2016)	0.66
"25, 2, 4 and 8 h, enabling less frequent blood sampling in further expanded pharmacokinetic studies for both AMR and AMR-OH."	( Simultaneous optimization of limited sampling points for pharmacokinetic analysis of amrubicin and amrubicinol in cancer patients. Hayashi, Y; Makihara, RA; Makino, Y; Nokihara, H; Ohe, Y; Sato, H; Sugiyama, E; Watanabe, M; Yamamoto, N, 2016)	0.66

Excerpt	Reference	Relevance
"A new anthracycline derivative, SM5887, in combination with commonly used anticancer agents was evaluated against T-cell leukemia MOLT-3 and human osteosarcoma MG-63 cell lines in culture."	( Effects of 13-hydroxy SM5887 in combination with other anticancer agents on human tumor cell lines. Kano, Y; Suzuki, K; Takagi, T; Yamauchi, Y; Yazawa, Y, 1996)	0.29
"A combination phase I study was conducted in a cohort of lung cancer patients to determine the maximum tolerated dose (MTD) and toxicities of irinotecan (CPT-11), a topoisomerase I inhibitor, in combination with amrubicin (AMR), a topoisomerase II inhibitor, and to observe their antitumor activities."	( A phase I study of irinotecan in combination with amrubicin for advanced lung cancer patients. Fukuoka, M; Kaneda, H; Kurata, T; Nakagawa, K; Tamura, K; Uejima, H, )	0.57
"We conducted a dose escalation study of Am in combination with CPT to determine the qualitative and quantitative toxicities and efficacy against extensive (ED) SCLC."	( Dose escalation study of amrubicin in combination with fixed-dose irinotecan in patients with extensive small-cell lung cancer. Oshita, F; Saito, H; Yamada, K, 2008)	0.65
"Amrubicin combined with carboplatin is quite effective for SCLC with acceptable toxic effects even for the elderly population."	( A phase II study of amrubicin combined with carboplatin for elderly patients with small-cell lung cancer: North Japan Lung Cancer Study Group Trial 0405. Fukuhara, T; Fukumoto, S; Harada, M; Harada, T; Inoue, A; Ishimoto, O; Kanbe, M; Maemondo, M; Nukiwa, T; Ogura, S; Oizumi, S; Sugawara, S; Suzuki, T; Usui, K; Yokouchi, H, 2010)	2.13
"The EORTC 08062 phase II randomised trial investigated the activity and safety of single agent amrubicin, cisplatin combined with amrubicin, and cisplatin combined with etoposide as first line treatment in extensive disease (ED) small cell lung cancer (SCLC)."	( Randomised phase II study of amrubicin as single agent or in combination with cisplatin versus cisplatin etoposide as first-line treatment in patients with extensive stage small cell lung cancer - EORTC 08062. Baas, P; Bosquee, L; Bustin, F; Dingemans, AM; Fink, C; Hasan, B; Konopa, K; Lorigan, P; Margerit, S; Marshall, E; O'Brien, ME; Stigt, JA; Van Meerbeeck, J, 2011)	0.88
" The objective of this study was to determine the recommended dose (RD) of amrubicin in combination with a fixed dose of cisplatin, and to assess the toxicity profile and feasibility of this regimen."	( Dose escalation and feasibility study of amrubicin combined with cisplatin in previously untreated patients with advanced non-small cell lung cancer. Asai, K; Hirata, K; Ichimaru, Y; Kimura, T; Kudoh, S; Kyoh, S; Mitsuoka, S; Tochino, Y; Yoshimura, N, 2013)	0.89
"Both amrubicin (Am) and S-1 are effective against non-small-cell lung cancer (NSCLC), and preclinical studies have demonstrated that the effect of tegafur/uracil, the original compound of S-1, in combination with Am significantly inhibits tumor growth."	( Phase I/II study of amrubicin in combination with S-1 as second-line chemotherapy for non-small-cell lung cancer without EGFR mutation. Kondo, T; Murakami, S; Oshita, F; Saito, H; Sugiura, M; Yamada, K, 2013)	1.23
"This is the first prospective study of AMR combined with CBDCA for refractory relapsed SCLC, which was effective and well tolerated."	( Phase II study of amrubicin combined with carboplatin for refractory relapsed small-cell lung cancer: North Japan Lung Cancer Group Trial 0802. Asahina, H; Harada, M; Hasegawa, Y; Inoue, A; Ishimoto, O; Kawashima, Y; Maemondo, M; Morikawa, N; Nukiwa, T; Oizumi, S; Okudera, K; Saito, R; Sakakibara, T; Sugawara, S; Suzuki, T; Usui, K, 2014)	0.74
"We conducted a phase I trial of erlotinib, an epidermal growth factor receptor tyrosine kinase inhibitor, combined with amrubicin, a topoisomerase II inhibitor."	( Phase I and pharmacokinetic study of erlotinib administered in combination with amrubicin in patients with previously treated, advanced non-small cell lung cancer. Asakuma, M; Fukui, T; Hamada, A; Hayashi, N; Hiyoshi, Y; Igawa, S; Ishihara, M; Kasajima, M; Katagiri, M; Katono, K; Kimura, M; Kubota, M; Maki, S; Masuda, N; Mitsufuji, H; Otani, S; Ryuge, S; Saito, H; Sasaki, J; Takakura, A; Toyooka, I; Wada, M; Yamamoto, M; Yokoba, M, 2015)	0.85
" No drug-drug interactions between erlotinib and amrubicin were observed in this study."	( Phase I and pharmacokinetic study of erlotinib administered in combination with amrubicin in patients with previously treated, advanced non-small cell lung cancer. Asakuma, M; Fukui, T; Hamada, A; Hayashi, N; Hiyoshi, Y; Igawa, S; Ishihara, M; Kasajima, M; Katagiri, M; Katono, K; Kimura, M; Kubota, M; Maki, S; Masuda, N; Mitsufuji, H; Otani, S; Ryuge, S; Saito, H; Sasaki, J; Takakura, A; Toyooka, I; Wada, M; Yamamoto, M; Yokoba, M, 2015)	0.9
"This phase 1 study investigated the safety of the anthracycline amrubicin combined with lenalidomide and dexamethasone in adults with relapsed or refractory multiple myeloma."	( A phase I, open-label, dose-escalation study of amrubicin in combination with lenalidomide and weekly dexamethasone in previously treated adults with relapsed or refractory multiple myeloma. Berube, C; Coutré, SE; Dinner, S; Dunn, TJ; Gotlib, J; Kaufman, GP; Liedtke, M; Medeiros, BC; Price, E, 2018)	0.98

Excerpt	Relevance	Reference
" The efficacy was assessed for 34 patients, excluding two patients: one who has not been followed up adequately and the other violated the dosing schedule (once per week)."	( [Early phase II clinical trial of amrubicin hydrochloride in patients with malignant lymphoma]. Ezaki, K; Hirano, M; Inoue, K; Kimura, I; Kuraishi, Y; Masaoka, T; Matsuda, T; Ogawa, M; Sanpi, K; Shibata, A; Shirakawa, S; Takagi, T; Tamura, K; Toki, H, 2001)	0.59
" Solutions containing anticancer agents at various concentrations were added followed by the addition of recombinant adenovirus solutions, and each IC50 was calculated based on the dose-response curves."	( Transfer of IkappaBalpha gene increase the sensitivity of paclitaxel mediated with caspase 3 activation in human lung cancer cell. Hara, N; Nakanishi, Y; Osaki, S; Pei, XH; Takayama, K; Ueno, H, 2003)	0.32
" The apparent total clearance of amrubicin showed a large interindividual variability, despite adjustment of dosage for body surface area."	( [Development of an individualized therapy for establishing the optimal dosage by the pharmacokinetics profiles of anticancer agents]. Hamada, A, 2005)	0.61
" Cisplatin was administered at a fixed dosage of 20 mg/m(2) while the administered dose of amrubicin was started at 20 mg/m(2)."	( Phase I study of amrubicin hydrochloride and cisplatin in patients previously treated for advanced non-small cell lung cancer. Ichinose, Y; Ikeda, J; Maruyama, R; Okamoto, T; Shoji, F; Wataya, H, 2006)	0.89
" There is a possibility that monitoring of the plasma concentrations of amrubicin and amrubicinol may provide an efficient tool for establishing the optimal dosage of amrubicin in each patient."	( Pharmacokinetics of amrubicin and its active metabolite amrubicinol in lung cancer patients. Hamada, A; Hira, A; Kishi, H; Matsumoto, M; Matsunaga, Y; Moriyama, E; Okamoto, I; Saito, H; Sasaki, J; Watanabe, H, 2006)	0.89
" Recommended dosage for previously untreated advanced NCSLC was 45 mg/m2/day by intravenous administration for 3 days."	( Amrubicin for non-small-cell lung cancer and small-cell lung cancer. Fukuoka, M; Kurata, T; Okamoto, I; Tamura, K, 2007)	1.78
"Between July 2003 and February 2009, a total of 27 patients were treated with AMR at a dosage of 40 mg x m(-2) x day(-1) on days 1-3 every 3 weeks."	( Clinical outcome of amrubicin therapy according to the prior chemotherapy sensitivities of extensive small cell lung cancer. Hirata, K; Kimura, T; Kudoh, S; Mitsuoka, S; Nagata, M; Suzumura, T; Tanaka, H; Ueda, T; Umekawa, K; Yoshimura, N, 2011)	0.69
" Due to the high incidence of febrile neutropenia, dosing was subsequently amended to 35 mg/m2 for the final 15 patients."	( Phase II trial of single agent amrubicin in patients with previously treated advanced thymic malignancies. Burns, M; Cunanan, KM; Gubens, MA; Hellyer, JA; Loehrer, PJ; Neal, JW; Padda, SK; Ramchandran, KJ; Riess, JW; San Pedro-Salcedo, M; Spittler, AJ; Wakelee, HA, 2019)	0.8

Role	Description
topoisomerase II inhibitor	null
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
prodrug	A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
quinone	Compounds having a fully conjugated cyclic dione structure, such as that of benzoquinones, derived from aromatic compounds by conversion of an even number of -CH= groups into -C(=O)- groups with any necessary rearrangement of double bonds (polycyclic and heterocyclic analogues are included).
tetracenes	Compounds containing a tetracene skeleton.
methyl ketone	A ketone of formula RC(=O)CH3 (R =/= H).
anthracycline antibiotic	An organic compound that has a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine and which exhibits antibiotic activity.
primary amino compound	A compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Assay ID	Title	Year	Journal	Article
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	6 (2.73)	18.7374
1990's	17 (7.73)	18.2507
2000's	66 (30.00)	29.6817
2010's	114 (51.82)	24.3611
2020's	17 (7.73)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	76 (33.04%)	5.53%
Reviews	25 (10.87%)	6.00%
Case Studies	29 (12.61%)	4.05%
Observational	0 (0.00%)	0.25%
Other	100 (43.48%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (20)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Multi-Center Phase 2 Trial of Single-Agent Amrubicin as Second-Line Therapy in Patients With Advanced/Metastatic Refractory Urothelial Carcinoma [NCT01331824]	Phase 2	22 participants (Actual)	Interventional	2011-02-28	Terminated(stopped due to due to a development decision by the funder)
A Phase I Study of Amrubicin and Cyclophosphamide in Patients With Advanced Solid Organ Malignancies [NCT00890955]	Phase 1	36 participants (Actual)	Interventional	2009-03-31	Completed
Randomized Phase II Study of Amrubicin as Single Agent or in Combination With Cisplatin Versus Etoposide-cisplatin as First-line Treatment in Patients With Extensive Stage SCLC (ES) [NCT00388960]	Phase 2	99 participants (Actual)	Interventional	2006-11-01	Completed
A Randomised, Open-Label Phase 3 Trial Comparing Amrubicin Versus Docetaxel in Patients With Non-Small Cell Lung Cancer After Failure of First-Line Chemotherapy [NCT01207011]	Phase 3	202 participants (Actual)	Interventional	2010-10-31	Completed
AMR PH GL 2007 CL001 Phase 3 A Randomized, Open-Label, Multinational Phase 3 Trial Comparing Amrubicin Versus Topotecan in Patients With Extensive or Limited and Sensitive or Refractory Small Cell Lung Cancer After Failure of First-Line Chemotherapy [NCT00547651]	Phase 3	637 participants (Actual)	Interventional	2007-09-01	Completed
A Phase 2 Trial of Single-Agent Amrubicin in Patients With Extensive Disease Small Cell Lung Cancer That is Refractory or Progressive Within 90 Days of Completion of First Line Platinum-based Chemotherapy [NCT00375193]	Phase 2	75 participants (Actual)	Interventional	2006-11-01	Completed
A Randomized Phase 2 Trial Comparing Amrubicin Versus Topotecan as Second-Line Treatment in Patients With Extensive Small Cell Lung Cancer Sensitive to First-Line Chemotherapy [NCT00319969]	Phase 2	76 participants (Actual)	Interventional	2006-04-30	Completed
Randomized Phase III Trial of Amrubicin Versus Carboplatin Plus Etoposide in Elderly Patients With Extensive-disease Small-cell Lung Cancer [NCT00286169]	Phase 3	130 participants (Anticipated)	Interventional	2006-04-30	Terminated
A Phase I Study to Assess the Safety, Pharmacokinetics, and Potential Effects of Amrubicin on the QT/QTc Interval in Cancer Patients With Advanced Solid Tumors. [NCT00915083]	Phase 1	24 participants (Actual)	Interventional	2009-06-01	Completed
An Open-Label, Randomized, Phase 2 Study Comparing TAS-102 Versus Topotecan or Amrubicin in Patients Requiring Second-Line Chemotherapy for Small Cell Lung Cancer That is Refractory or Sensitive to First-Line Platinum-Based Chemotherapy [NCT01904253]	Phase 2	18 participants (Actual)	Interventional	2013-07-31	Terminated(stopped due to The preliminary data does not suggest any safety signal, but an ad hoc interim analysis showed an imbalance of PFS between the two arms)
A Phase 2 Trial of Amrubicin With or Without Herceptin in the Treatment of Metastatic Breast Cancer [NCT00380835]	Phase 2	66 participants (Anticipated)	Interventional		Withdrawn(stopped due to Study Never Initiated)
Phase I/II Trial of Amrubicin as Second- or Third-Line Treatment for Patients With HER2-Negative Metastatic Breast Cancer [NCT01033032]	Phase 1/Phase 2	78 participants (Actual)	Interventional	2009-12-31	Completed
A Phase II Trial of Amrubicin and Carboplatin With Pegfilgrastim in Patients With Extensive-Stage Small Cell Lung Cancer [NCT01076504]	Phase 2	81 participants (Actual)	Interventional	2009-12-31	Completed
Phase I Study of Weekly Irinotecan Combined With Amrubicin in Previously Treated Small-Cell Lung Cancer [NCT00132054]	Phase 1	30 participants (Anticipated)	Interventional	2004-05-31	Completed
Randomized, Open-label, phase3 Trial Comparing Amrubicin Combined With Cisplatin Versus Etoposide-Cisplatin as First-line Treatment in Patients With Extensive Disease SCLC [NCT00660504]	Phase 3	300 participants (Actual)	Interventional	2008-04-30	Completed
A Phase II Study of Amrubicin Chemotherapy as First Line Treatment in Patients With Metastatic or Unresectable Soft Tissue Sarcoma [NCT01259375]	Phase 2	24 participants (Actual)	Interventional	2011-09-30	Completed
An Open-label, Randomized, Phase 3 Study of Nivolumab or Chemotherapy in Subjects With Relapsed Small-cell Lung Cancer After Platinum-based First Line Chemotherapy (CheckMate 331: CHECKpoint Pathway and nivoluMAb Clinical Trial Evaluation 331) [NCT02481830]	Phase 3	569 participants (Actual)	Interventional	2015-09-14	Completed
A Randomized, Open-label, Phase 3 Study of Tarlatamab Compared With Standard of Care in Subjects With Relapsed Small Cell Lung Cancer After Platinum-based First-line Chemotherapy [NCT05740566]	Phase 3	700 participants (Anticipated)	Interventional	2023-05-31	Recruiting
A Phase II Study of Amrubicin in Relapsed or Refractory Thymic Malignancies [NCT01364727]	Phase 2	33 participants (Actual)	Interventional	2011-06-30	Completed
A Phase 1 Study of Amrubicin in Combination With Lenalidomide and Weekly Dexamethasone in Relapsed/Refractory Multiple Myeloma [NCT01355705]	Phase 1/Phase 2	14 participants (Actual)	Interventional	2011-08-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00660504 (4) [back to overview]	Overall Survival at 6 and 12 Months
NCT00660504 (4) [back to overview]	Objective Response Rate
NCT00660504 (4) [back to overview]	Overall Survival
NCT00660504 (4) [back to overview]	Progression-Free Survival
NCT01033032 (4) [back to overview]	Number of Patients With Adverse Events as a Measure of Safety and Tolerability
NCT01033032 (4) [back to overview]	Overall Response Rate (ORR)
NCT01033032 (4) [back to overview]	Overall Survival (OS) of MTD/Phase II Patients
NCT01033032 (4) [back to overview]	Progression-Free Survival (PFS) of MTD/Phase II Patients
NCT01076504 (5) [back to overview]	1-year Survival
NCT01076504 (5) [back to overview]	Objective Response Rate
NCT01076504 (5) [back to overview]	Overall Survival
NCT01076504 (5) [back to overview]	Time to Progression
NCT01076504 (5) [back to overview]	Toxicity/Safety
NCT01259375 (5) [back to overview]	Number of Participants With Serious Adverse Events
NCT01259375 (5) [back to overview]	Overall Survival
NCT01259375 (5) [back to overview]	Progression Free Survival
NCT01259375 (5) [back to overview]	Response Rate for Amrubicin in Patients With Metastatic or Advanced Sarcoma as First Line Therapy.
NCT01259375 (5) [back to overview]	Differential Response to Amurbicin Among Certain Histologic Subtypes of Sarcoma.
NCT01331824 (4) [back to overview]	Safety as Measured by the Frequency and Type of Adverse Events as Per the Common Terminology for Adverse Events (CTCAE) Version 4.0.
NCT01331824 (4) [back to overview]	Objective Response Rate as Measured by Response Evaluation Criteria in Solid Tumors (RECIST 1.1)
NCT01331824 (4) [back to overview]	Overall Survival
NCT01331824 (4) [back to overview]	Progression-free Survival
NCT01355705 (4) [back to overview]	Duration of Response (DOR)
NCT01355705 (4) [back to overview]	Progression-free Survival (PFS)
NCT01355705 (4) [back to overview]	Time-to-next Treatment
NCT01355705 (4) [back to overview]	Response Rates After Amrubicin + Lenalidomide + Dexamethasone, Per International Myeloma Working Group Uniform Response Criteria
NCT01364727 (3) [back to overview]	Median Progression-free Survival (PFS)
NCT01364727 (3) [back to overview]	Disease Control Rate (DCR)
NCT01364727 (3) [back to overview]	Overall Response Rate (ORR)
NCT02481830 (4) [back to overview]	Objective Response Rate (ORR)
NCT02481830 (4) [back to overview]	Overall Survival (OS)
NCT02481830 (4) [back to overview]	Overall Survival (OS) - Extended Collection
NCT02481830 (4) [back to overview]	Progression Free Survival (PFS)

Overall Survival at 6 and 12 Months

(NCT00660504)
Timeframe: 6 and 12 months.

Intervention	percentage of patients (Number)
	6-month	12-month
Amrubicin Combined With Cisplatin Group	89.26	48.59
Etoposide Combined With Cisplatin Group	86.00	41.93

Intervention	percentage of participants (Number)
Amrubicin Combined With Cisplatin Group	69.80
Etoposide Combined With Cisplatin Group	57.33

Intervention	month (Median)
Amrubicin Combined With Cisplatin Group	11.79
Etoposide Combined With Cisplatin Group	10.28

Intervention	month (Median)
Amrubicin Combined With Cisplatin Group	6.83
Etoposide Combined With Cisplatin Group	5.72

Intervention	participants (Number)
	Anemia	Leukopenia	Thrombocytopenia	Neutropenia	Febrile neutropenia	Hypokalemia	Fatigue	Dehydration	Infection	Hyponatremia	Nausea	Vomiting	Hyperglycemia	Muscle weakness	Thrombosis/embolism
Amrubicin/Carboplatin With Pegfilgrastim	22	30	36	29	10	14	11	8	11	10	8	6	3	4	3

Intervention	participants (Number)
	liposarcoma	myxoid liposarcoma with TLS-CHOP translocation	leiomyoscarcoma
All Groups	1	1	1

Intervention	percentage of participants (Number)
	Complete Response (CR) rate	Very Good Partial Response (VGPR) Rate	Total CR + VGPR	Partial Response (PR) Rate	Overall Response Rate (ORR = CR + VGPR + PR)
Amrubicin + Lenalidomide + Dexamethasone	0	7.6	7.6	15.4	23

Intervention	Participants (Count of Participants)
	Overall Response Rate (ORR)	Stable Disease (SD)	Disease control rate (DCR)
Amrubicin	6	23	29

Intervention	Participants (Count of Participants)
	Complete Response (CR)	Partial Response (PR)	Overall response rate (ORR)
Amrubicin	0	6	6

Substance	Relationship Strength	Studies	Trials	Classes	Roles
thymine [no description available]	4.43	1	1	pyrimidine nucleobase; pyrimidone	Escherichia coli metabolite; human metabolite; mouse metabolite
uracil 2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder	4.78	2	1	pyrimidine nucleobase; pyrimidone	allergen; Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; prodrug; Saccharomyces cerevisiae metabolite
verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.	2.47	2	0	aromatic ether; nitrile; polyether; tertiary amino compound
disopyramide Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug.	3.41	1	1	monocarboxylic acid amide; pyridines; tertiary amino compound	anti-arrhythmia drug
fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.	3.1	1	0	nucleobase analogue; organofluorine compound	antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source	2.1	1	0	chromones; morpholines; organochlorine compound	autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector
mitoxantrone Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.	7.07	1	0	dihydroxyanthraquinone	analgesic; antineoplastic agent
oxonic acid Oxonic Acid: Antagonist of urate oxidase.	4.94	2	1	1,3,5-triazines; monocarboxylic acid
tegafur [no description available]	5.22	3	1	organohalogen compound; pyrimidines
temozolomide [no description available]	2.21	1	0	imidazotetrazine; monocarboxylic acid amide; triazene derivative	alkylating agent; antineoplastic agent; prodrug
thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.	7.6	4	4	phthalimides; piperidones
prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.	3.39	1	1	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic
trifluridine Trifluridine: An antiviral derivative of THYMIDINE used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to HERPES SIMPLEX virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557). trifluridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-trifluoromethyluracil as the nucleobase. An antiviral drug used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis.	4.43	1	1	nucleoside analogue; organofluorine compound; pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent; antiviral drug; EC 2.1.1.45 (thymidylate synthase) inhibitor
quinazolines Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.	5.22	3	1	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines
oxazoles Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.	2.01	1	0	1,3-oxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
thiazoles [no description available]	2.73	3	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
pyrazines Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.	3.12	1	0	diazine; pyrazines	Daphnia magna metabolite
deoxycytidine [no description available]	3.53	2	0	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
platinum Platinum: A heavy, soft, whitish metal, resembling tin, with atomic number 78, atomic weight 195.084, symbol Pt. It is used in manufacturing equipment for laboratory and industrial use. It occurs as a black powder (platinum black) and as a spongy substance (spongy platinum) and may have been known in Pliny's time as alutiae.	5.19	3	1	elemental platinum; nickel group element atom; platinum group metal atom
camptothecin NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source	10.83	27	10	delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite
daunorubicin Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.	2.4	2	0	aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones	antineoplastic agent; bacterial metabolite
razoxane Razoxane: An antimitotic agent with immunosuppressive properties.	7.07	1	0	N-alkylpiperazine
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	11.62	8	2	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
etoposide [no description available]	11.37	22	6	beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound	antineoplastic agent; DNA synthesis inhibitor
epirubicin Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA.	2.97	4	0	aminoglycoside; anthracycline antibiotic; anthracycline; deoxy hexoside; monosaccharide derivative; p-quinones; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	antimicrobial agent; antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
idarubicin Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA.	4.46	1	1	anthracycline antibiotic; deoxy hexoside; monosaccharide derivative
topotecan Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.	10.47	12	6	pyranoindolizinoquinoline	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor
gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.	3.53	2	0	organofluorine compound; pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic
irinotecan [no description available]	10.87	28	10	carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug
acridine orange Acridine Orange: A cationic cytochemical stain specific for cell nuclei, especially DNA. It is used as a supravital stain and in fluorescence cytochemistry. It may cause mutations in microorganisms.. acridine orange : Fluorescent dye useful for cell cycle determination. It is cell-permeable, and interacts with DNA and RNA by intercalation or electrostatic attractions respectively.. acridine orange free base : A member of the class of aminoacridines that is acridine carrying two dimethylamino substituents at positions 3 and 6. The hydrochloride salt is the fluorescent dye 'acridine orange', used for cell cycle determination.	2.01	1	0	aminoacridines; aromatic amine; tertiary amino compound	fluorochrome; histological dye
thiazolyl blue thiazolyl blue: RN & II refers to bromide. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide : The bromide salt of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium.	2.73	3	0	organic bromide salt	colorimetric reagent; dye
kt 6149 KW 2149: derivative of mitomycin C; structure in first source	1.97	1	0
me 2303 ME 2303: structure given in first source; RN given refers to (2S-cis)-isomer	5.67	3	1
imatinib mesylate imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.	8.53	2	0	methanesulfonate salt	anticoronaviral agent; antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor
gefitinib [no description available]	3.53	2	0	aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound	antineoplastic agent; epidermal growth factor receptor antagonist
fr 66973 FR 66973: antitumor antibiotic from Streptomyces sandaensis; more potent against B16 melanoma & P388 leukemia than mitomycin C; structure given in first source	1.97	1	0
10-propargyl-10-deazaaminopterin 10-propargyl-10-deazaaminopterin: structure in first source. pralatrexate : A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma.	3.17	1	0	N-acyl-L-glutamic acid; pteridines; terminal acetylenic compound	antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor
docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.	5.07	3	1	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent
sabarubicin sabarubicin: structure given in first source	2.15	1	0
jte 522 tiracoxib: The combined administration of tiracoxib with probucol significantly inhibited the tumor growth. The angiogenesis was markedly reduced; no further information available 1/31/2001. tilmacoxib : A member of the class of 1,3-oxazoles that is that is 1,3-oxazole which is substituted at positions 2, 4 and 5 by methyl, cyclohexyl, and 3-fluoro-4-sulfamoylphenyl groups, respectively.	2.01	1	0	1,3-oxazoles; organofluorine compound; sulfonamide	cyclooxygenase 2 inhibitor
aminopterin Aminopterin: A folic acid derivative used as a rodenticide that has been shown to be teratogenic.	3.17	1	0	dicarboxylic acid	EC 1.5.1.3 (dihydrofolate reductase) inhibitor; mutagen
erlotinib hydrochloride [no description available]	4.94	2	1	hydrochloride; terminal acetylenic compound	antineoplastic agent; protein kinase inhibitor
lenalidomide [no description available]	7.6	4	4	aromatic amine; dicarboximide; isoindoles; piperidones	angiogenesis inhibitor; antineoplastic agent; immunomodulator
nogalamycin Nogalamycin: An anthrocycline from a Streptomyces nogalater variant. It is a cytolytic antineoplastic that inhibits DNA-dependent RNA synthesis by binding to DNA.. nogalamycin : An anthracycline antibiotic isolated from Streptomyces nogalater. It is a DNA intercalator and exhibits anticancer properties.	1.97	1	0
menogaril Menogaril: A semisynthetic anthracycline with the amino sugar on the D ring. It displays broad-spectrum antineoplastic activity against a variety of tumors.	5.66	3	1
bortezomib [no description available]	3.12	1	0	amino acid amide; L-phenylalanine derivative; pyrazines	antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor
carboplatin [no description available]	10.13	23	11
thiourea Thiourea: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.. thiourea : The simplest member of the thiourea class, consisting of urea with the oxygen atom substituted by sulfur.	2.21	1	0	one-carbon compound; thioureas; ureas	antioxidant; chromophore
picromycin picromycin: structure. pikromycin : A macrolide antibiotic that is biosynthesised by Streptomyces venezuelae.	2.15	1	0	enone; macrolide antibiotic; monosaccharide derivative	bacterial metabolite
morpholinoanthracycline mx2 morpholinoanthracycline MX2: structure given in first source	5.15	3	1
mp470 [no description available]	2.21	1	0	N-arylpiperazine
pirarubicin [no description available]	2.01	1	0	anthracycline
amrubicinol amrubicinol: a diastereoisomeric mixture; a synthetic antracycline drug. amrubicinol : A diastereoisomeric mixture resulting from the formal reduction of the acetyl group at position 9 of amrubicin to the corresponding 1-hydroxyethyl group. The active metabolite of amrubicin in lung cancer patients.	7.08	23	4	diastereoisomeric mixture; quinone; secondary alcohol; tetracenes	antineoplastic agent; apoptosis inducer; topoisomerase II inhibitor
pituitrin Pituitrin: A substance or extract from the neurohypophysis (PITUITARY GLAND, POSTERIOR).	2.25	1	0
interleukin-8 Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.	2.03	1	0
s 1 (combination) S 1 (combination): consists of tegafur, 5-chloro-2,4-dihydroxyuridine & potassium oxonate; an inhibitor of fluorouracil(5-FU) degradation; prolongs the blood 5-FU level as well as increases selective toxicity to tumor; used for the treatment of colon cancer	4.94	2	1
carubicin Carubicin: A very toxic anthracycline-type antineoplastic related to DAUNORUBICIN, obtained from Actinomadura carminata.. carminomycin(1+) : An anthracyline cation that is the conjugate acid of carminomycin, obtained by protonation of the amino group.	5.15	3	1	anthracycline cation
nedaplatin nedaplatin: structure given in first source	8.48	1	1
sc002 SC002: structure in first source	2.21	1	0
deoxyguanosine [no description available]	2.02	1	0	purine 2'-deoxyribonucleoside; purines 2'-deoxy-D-ribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
guanine [no description available]	3.55	2	0	2-aminopurines; oxopurine; purine nucleobase	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
pemetrexed pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT).	8.55	2	0	N-acyl-L-glutamic acid; pyrrolopyrimidine	antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; EC 2.1.1.45 (thymidylate synthase) inhibitor; EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor
8-hydroxy-2'-deoxyguanosine 8-Hydroxy-2'-Deoxyguanosine: Common oxidized form of deoxyguanosine in which C-8 position of guanine base has a carbonyl group.. 8-hydroxy-2'-deoxyguanosine : Guanosine substituted at the purine 8-position by a hydroxy group. It is used as a biomarker of oxidative DNA damage.	2.02	1	0	guanosines	biomarker

amrubicin

Description

Cross-References

Synonyms (35)

Research Excerpts

Overview

Effects

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Dosage Studied

Roles (3)

Drug Classes (5)

Bioassays (1)

Research

Studies (220)

Market Indicators

Research Demand Index: 31.19

Study Types

Clinical Trials (20)

Trial Overview

Trial Outcomes

Overall Survival at 6 and 12 Months

Objective Response Rate

Overall Survival

Progression-Free Survival

Number of Patients With Adverse Events as a Measure of Safety and Tolerability

Overall Response Rate (ORR)

Overall Survival (OS) of MTD/Phase II Patients

Progression-Free Survival (PFS) of MTD/Phase II Patients

1-year Survival

Objective Response Rate

Overall Survival

Time to Progression

Toxicity/Safety

Number of Participants With Serious Adverse Events

Overall Survival

Progression Free Survival

Response Rate for Amrubicin in Patients With Metastatic or Advanced Sarcoma as First Line Therapy.

Differential Response to Amurbicin Among Certain Histologic Subtypes of Sarcoma.

Safety as Measured by the Frequency and Type of Adverse Events as Per the Common Terminology for Adverse Events (CTCAE) Version 4.0.

Objective Response Rate as Measured by Response Evaluation Criteria in Solid Tumors (RECIST 1.1)

Overall Survival

Progression-free Survival

Duration of Response (DOR)

Progression-free Survival (PFS)

Time-to-next Treatment

Response Rates After Amrubicin + Lenalidomide + Dexamethasone, Per International Myeloma Working Group Uniform Response Criteria

Median Progression-free Survival (PFS)

Disease Control Rate (DCR)

Overall Response Rate (ORR)

Objective Response Rate (ORR)

Overall Survival (OS)

Overall Survival (OS) - Extended Collection

Progression Free Survival (PFS)

Related Drugs (63)

Related Conditions (159)