Pharmacokinetics and tissue distribution of idarubicin and its active metabolite idarubicinol in the rabbit.

Abstract:

:A three-compartment model was fitted to idarubicin data in a NONMEM pooled-data approach. Clearance (CL) of 221.7 ml/min was relatively high, and drug distribution was rapid (CLD = 248.3 ml/min) and extensive [steady-state volume of distribution (Vss) 24 1]. The area under the concentration-time curve (AUC) of idarbicinol was 8 times that of idarubicin. Concentrations of idarubicin (idarubicinol) measured in the myocardium at 24 h after i.v. administration of idarubicin were 20 (5) times those determined in plasma. Tissue concentrations of idarubicinol were up to 400 times those of idarubicin, indicating that the active metabolite contributes significantly to the overall drug action.

authors

Looby M,Linke R,Weiss M

doi

10.1007/s002800050614

subject

Has Abstract

pub_date

1997-01-01 00:00:00

pages

554-6

issue

6

eissn

0344-5704

issn

1432-0843

journal_volume

39

pub_type

杂志文章
  • Tumor resensitization to erlotinib following brief substitution of cetuximab.

    abstract::Targeted inhibition of epidermal growth factor receptors (EGFR) is becoming a standard anticancer treatment in defined clinical scenarios. EGFR inhibition may be achieved either by small-molecule orally bioavailable tyrosine kinase inhibitors, such as gefitinib or erlotinib, or else by large-molecule receptor antibodi...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-008-0698-6

    authors: Epstein RJ,Leung TW

    更新日期:2008-11-01 00:00:00

  • Ifosfamide in advanced epidermoid head and neck cancer.

    abstract::A total of 37 men with epidermoid head and neck cancer whose disease had recurred following primary treatment (surgery and/or radiotherapy) received first-line chemotherapy with ifosfamide at i.v. doses of 3 g/m2 given daily on 3 consecutive days in combination with mesna (600 mg/m2 x 3 oral daily doses on days 1-3) e...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00685683

    authors: Martín M,Diaz-Rubio E,González Larriba JL,Casado A,Sastre J,López-Vega JM,Almenarez J,Dominguez S

    更新日期:1993-01-01 00:00:00

  • Phase II clinical trial of PM00104 (Zalypsis(®)) in urothelial carcinoma patients progressing after first-line platinum-based regimen.

    abstract:PURPOSE:This exploratory phase II clinical trial evaluated the antitumor activity, safety profile and pharmacokinetics of PM00104 (Zalypsis(®)) 3 mg/m(2) 1 h every 3-week intravenous infusion in patients with advanced and/or metastatic urothelial carcinoma progressing after first-line platinum-based chemotherapy. METH...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-014-2419-7

    authors: Castellano DE,Bellmunt J,Maroto JP,Font-Pous A,Morales-Barrera R,Ghanem I,Suarez C,Martín Lorente C,Etxaniz O,Capdevila L,Coronado C,Alfaro V,Siguero M,Fernández-Teruel C,Carles J

    更新日期:2014-04-01 00:00:00

  • Clinical pharmacology of UCN-01: initial observations and comparison to preclinical models.

    abstract::UCN-01 (7-hydroxystaurosporine; NSC 638850) is a protein kinase antagonist selected for clinical trial based in part on evidence of efficacy in a preclinical renal carcinoma xenograft model. Schedule studies and in vitro studies suggested that a 72-h continuous infusion would be appropriate. In rats and dogs, maximum ...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s002800051080

    authors: Sausville EA,Lush RD,Headlee D,Smith AC,Figg WD,Arbuck SG,Senderowicz AM,Fuse E,Tanii H,Kuwabara T,Kobayashi S

    更新日期:1998-01-01 00:00:00

  • Safety and pharmacokinetics of S-1 in a recurrent colon cancer patient with chronic myeloid leukemia treated with dasatinib: a case report.

    abstract:PURPOSE:The safety of S-1 in recurrent colorectal cancer patients with chronic myeloid leukemia (CML) treated with dasatinib has not been established. We evaluated the safety and pharmacokinetics of S-1 in a recurrent colon cancer patient with CML treated with dasatinib. PATIENT:A 70-year-old man had undergone surgery...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-014-2620-8

    authors: Sueda T,Kudo T,Sakai D,Uemura M,Nishimura J,Hata T,Takemasa I,Mizushima T,Yamamoto H,Ezoe S,Matsumoto K,Doki Y,Mori M,Satoh T

    更新日期:2014-12-01 00:00:00

  • Phase I, dose escalation and pharmacokinetic study of cediranib (RECENTIN), a highly potent and selective VEGFR signaling inhibitor, in Japanese patients with advanced solid tumors.

    abstract:PURPOSE:To evaluate safety and tolerability of cediranib, a highly potent and selective vascular endothelial growth factor signaling inhibitor, in Japanese patients with advanced solid tumors refractory to standard therapies. METHODS:In part A (n = 16), patients received once-daily oral cediranib (10-45 mg) to identif...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-009-0979-8

    authors: Yamamoto N,Tamura T,Yamamoto N,Yamada K,Yamada Y,Nokihara H,Fujiwara Y,Takahashi T,Murakami H,Boku N,Yamazaki K,Puchalski TA,Shin E

    更新日期:2009-11-01 00:00:00

  • Antitumor activity and cytotoxicity of a new ankinomycin derivative, 3'-,11-dibutyryl ankinomycin.

    abstract::Ankinomycin is a new antitumor antibiotic found in the culture broth of Streptomyces sp. SF2587. Ankinomycin showed marked cytotoxicity and antitumor activity against some murine leukemias, but the activity against murine solid tumors was rather weak because of its strong acute toxicity. We synthesized ankinomycin acy...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00685831

    authors: Ishii S,Satoh Y,Tsuruo T

    更新日期:1993-01-01 00:00:00

  • Phase II study of FOLFIRI regimen in patients with advanced colorectal cancer refractory to fluoropyrimidine and oxaliplatin.

    abstract:PURPOSE:To evaluate the efficacy and safety of FOLFIRI regimen in patients with advanced colorectal cancer refractory to fluoropyrimidine and oxaliplatin. METHODS:The FOLFIRI regimen consisted of intravenous infusion of irinotecan 180 mg/m(2) on day 1 plus leucovorin (LV) 400 mg/m(2) on day 1 plus 5-fluorouracil (5-FU...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-010-1301-5

    authors: Bao HY,Fang WJ,Zhang XC,Shi GM,Huang S,Yu LF,Chen J,Mou HB,Deng J,Shen P,Xu N

    更新日期:2011-01-01 00:00:00

  • Ineligibility for the PACIFIC trial in unresectable stage III non-small cell lung cancer patients.

    abstract:PURPOSE:Recently, based on results of the PACIFIC trial, durvalumab after chemoradiotherapy (CRT) became the standard therapy for unresectable stage III non-small cell lung cancer (NSCLC). However, in the PACIFIC trial, patients were recruited and randomized after CRT, and certain patients were considered ineligible af...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-019-03885-4

    authors: Hosoya K,Fujimoto D,Kawachi H,Sato Y,Kogo M,Nagata K,Nakagawa A,Tachikawa R,Hiraoka S,Kokubo M,Tomii K

    更新日期:2019-08-01 00:00:00

  • Activity of fenretinide plus chemotherapeutic agents in small-cell lung cancer cell lines.

    abstract:PURPOSE:Fenretinide [N-(4-hydroxyphenyl)retinamide, 4HPR], a synthetic retinoid, is a potent inducer of apoptosis in small-cell lung cancer (SCLC) cell lines that may act through the generation of reactive oxygen species, suggesting that it may enhance the activity of other cytotoxic agents. In light of 4HPR's clinical...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002800050875

    authors: Kalemkerian GP,Ou X

    更新日期:1999-01-01 00:00:00

  • Hypersensitivity reactions to deoxycoformycin.

    abstract::Deoxycoformycin (dCF) is a promising new antineoplastic agent in the treatment of lymphoid malignancies, particularly hairy cell leukemia (HCL). Skin toxicity in the form of a maculopapular eruption has previously been reported but has not clearly been associated with idiosyncratic reactions. We present five cases of ...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00267950

    authors: O'Dwyer PJ,King SA,Eisenhauer E,Grem JL,Hoth DF

    更新日期:1989-01-01 00:00:00

  • CDDO-Me, a synthetic triterpenoid, inhibits expression of IL-6 and Stat3 phosphorylation in multi-drug resistant ovarian cancer cells.

    abstract::Previous studies have identified interleukin 6 (IL-6) as an important cytokine with prognostic significance in ovarian cancer. Activation of the IL-6-Stat3 pathway contributes to tumor cell growth, survival and drug resistance in several cancers, including ovarian cancer. To explore potential therapeutic strategies fo...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-008-0785-8

    authors: Duan Z,Ames RY,Ryan M,Hornicek FJ,Mankin H,Seiden MV

    更新日期:2009-03-01 00:00:00

  • Translational research of a novel humanized epidermal growth factor receptor-related protein: a putative inhibitor of pan-ErbB.

    abstract:PURPOSE:The ErbB family members are protein tyrosine kinases, which play a crucial role in the signal transduction pathways that regulate key cellular functions. Overexpression of the ErbB family members is associated with oncogenicity, metastatic potential, cell proliferation, apoptosis, angiogenesis, and prognosis in...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1007/s00280-011-1748-z

    authors: Fu XH,Li J,Huang JJ,Zheng S,Zhang SZ

    更新日期:2011-12-01 00:00:00

  • Pharmacodynamic and DNA methylation studies of high-dose 1-beta-D-arabinofuranosyl cytosine before and after in vivo 5-azacytidine treatment in pediatric patients with refractory acute lymphocytic leukemia.

    abstract::The primary development of clinical resistance to 1-beta-D-arabinofuranosyl cytosine (ara-C) in leukemic blast cells is expressed as decreased cellular concentrations of its active anabolite. Correlations exist between the cellular concentrations of 1-beta-D-arabinofuranosyl cytosine 5'-triphosphate (ara-CTP) in leuke...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00257619

    authors: Avramis VI,Mecum RA,Nyce J,Steele DA,Holcenberg JS

    更新日期:1989-01-01 00:00:00

  • The stability of ifosfamide in aqueous solution and its suitability for continuous 7-day infusion by ambulatory pump.

    abstract::Dose fractionation is known to reduce the toxicity of ifosfamide and also results in an increased production of alkylating metabolites. Administration by slow infusion using the convenience of ambulatory pumps is therefore of interest. We used HPLC to investigate the stability of ifosfamide in aqueous solution (either...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02897261

    authors: Radford JA,Margison JM,Swindell R,Lind MJ,Wilkinson PM,Thatcher N

    更新日期:1990-01-01 00:00:00

  • A phase I study of resminostat in Japanese patients with advanced solid tumors.

    abstract:PURPOSE:This study was performed to evaluate the safety and determine the recommended dose (RD) of resminostat monotherapy, an oral histone deacetylase (HDAC) inhibitor, in Japanese patients with advanced solid tumors. METHODS:Resminostat was administered to patients with advanced solid tumors on a 14-day cycle consis...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-015-2741-8

    authors: Kitazono S,Fujiwara Y,Nakamichi S,Mizugaki H,Nokihara H,Yamamoto N,Yamada Y,Inukai E,Nakamura O,Tamura T

    更新日期:2015-06-01 00:00:00

  • Melanoma vaccines: the paradox of T cell activation without clinical response.

    abstract::In recent years significant progress in the understanding of the immune biology of melanoma has evolved from the identification of melanoma antigens (MAs) recognized by T cells. MAs consist of intracellular proteins that are expressed on the surface of cancer cells in association with human leukocyte antigen (HLA) cla...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1007/pl00014052

    authors: Nielsen MB,Marincola FM

    更新日期:2000-01-01 00:00:00

  • Combination chemotherapy for advanced urothelial-tract carcinoma.

    abstract::Between December 1982 and November 1990, 31 patients with advanced urothelial carcinoma were treated with one of two combination chemotherapy regimens. A total of 20 patients were treated with 3 mg/m2 mitomycin C and 300 mg/m2 cyclophosphamide given intravenously every 10-14 days and with 180 mg/m2 5-fluorouracil (5-F...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00686944

    authors: Sahashi M,Ono Y,Matsuura O,Ohshima S,Fukushima M

    更新日期:1992-01-01 00:00:00

  • Preclinical pharmacologic evaluation of geldanamycin as an antitumor agent.

    abstract::The plasma pharmacokinetics of the anti-tumor antibiotic geldanamycin (GM: NSC 122750), a naturally occurring benzoquinoid ansamycin, was characterized in mice and a beagle dog. Concentrations of GM well above 0.1 microgram/ml, which was typically effective against neoplastic cell lines responsive to the drug in vitro...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00689048

    authors: Supko JG,Hickman RL,Grever MR,Malspeis L

    更新日期:1995-01-01 00:00:00

  • ABCC4 functional SNP in the 3' splice acceptor site of exon 8 (G912T) is associated with unfavorable clinical outcome in children with acute lymphoblastic leukemia.

    abstract:OBJECTIVES:ATP-binding cassette subfamily C member 4 (ABCC4) encoding MRP4 protein is involved in pediatric acute lymphoblastic leukemia (ALL) drug resistance. The nonsynonymous single nucleotide polymorphism (SNP) rs2274407 (G912T; K304N) is located in the 3' splice acceptor site of exon 8 of ABCC4 pre-mRNA. The aim o...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-017-3340-7

    authors: Mesrian Tanha H,Rahgozar S,Mojtabavi Naeini M

    更新日期:2017-07-01 00:00:00

  • Marimastat (BB2516): current status of development.

    abstract::Marimastat (BB-2516) is the first matrix metalloproteinase inhibitor to have entered clinical trials in the field of oncology. It has excellent bioavailability and has completed phase I and II trials. Phase I studies involved healthy volunteers who received short courses of marimastat; these were well tolerated. Sympt...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章,评审

    doi:10.1007/s002800051099

    authors: Steward WP

    更新日期:1999-01-01 00:00:00

  • Phase I dose escalation study of temsirolimus in combination with metformin in patients with advanced/refractory cancers.

    abstract:PURPOSE:Mammalian target of rapamycin (mTOR) inhibitors like temsirolimus may result in undesirable AKT upregulation. Metformin inhibits mTOR through different mechanisms and may enhance temsirolimus's antitumor activity. We conducted an open-label phase I dose escalation trial of this drug combination in patients with...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-016-3009-7

    authors: Khawaja MR,Nick AM,Madhusudanannair V,Fu S,Hong D,McQuinn LM,Ng CS,Piha-Paul SA,Janku F,Subbiah V,Tsimberidou A,Karp D,Meric-Bernstam F,Lu KH,Naing A

    更新日期:2016-05-01 00:00:00

  • Intravenous 5-fluoro-2'-deoxycytidine administered with tetrahydrouridine increases the proportion of p16-expressing circulating tumor cells in patients with advanced solid tumors.

    abstract:PURPOSE:Following promising responses to the DNA methyltransferase (DNMT) inhibitor 5-fluoro-2'-deoxycytidine (FdCyd) combined with tetrahydrouridine (THU) in phase 1 testing, we initiated a non-randomized phase 2 study to assess response to this combination in patients with advanced solid tumor types for which tumor s...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-020-04073-5

    authors: Coyne GO',Wang L,Zlott J,Juwara L,Covey JM,Beumer JH,Cristea MC,Newman EM,Koehler S,Nieva JJ,Garcia AA,Gandara DR,Miller B,Khin S,Miller SB,Steinberg SM,Rubinstein L,Parchment RE,Kinders RJ,Piekarz RL,Kummar S,C

    更新日期:2020-05-01 00:00:00

  • Brain tumor-targeted delivery and therapy by focused ultrasound introduced doxorubicin-loaded cationic liposomes.

    abstract::Brain tumor lacks effective delivery system for treatment. Focused ultrasound (FUS) can reversibly open BBB without impacts on normal tissues. As a potential drug carrier, cationic liposomes (CLs) have the ability to passively accumulate in tumor tissues for their positive charge. In this study, FUS introduced doxorub...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-015-2926-1

    authors: Lin Q,Mao KL,Tian FR,Yang JJ,Chen PP,Xu J,Fan ZL,Zhao YP,Li WF,Zheng L,Zhao YZ,Lu CT

    更新日期:2016-02-01 00:00:00

  • Phase II trial of gemcitabine combined with cisplatin in patients with inoperable biliary tract carcinomas.

    abstract:OBJECTIVES:The aim of this phase II study was to evaluate the response rate to gemcitabine combined with cisplatin in patients with locally advanced, metastatic or recurrent biliary tract cancer who had received no prior chemotherapy. METHODS:The treatment consisted of cisplatin 70 mg/m(2) in intravenous infusion foll...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章,多中心研究

    doi:10.1007/s00280-007-0444-5

    authors: Lee J,Kim TY,Lee MA,Ahn MJ,Kim HK,Lim HY,Lee NS,Park BJ,Kim JS,Korean Cancer Study Group.

    更新日期:2008-01-01 00:00:00

  • Phase II and pharmacokinetic/pharmacodynamic trial of sequential topoisomerase I and II inhibition with topotecan and etoposide in advanced non-small-cell lung cancer.

    abstract:PURPOSE:In vitro and in vivo preclinical models have demonstrated synergistic activity when topoisomerase I and II inhibitors are administered sequentially. Topoisomerase I inhibitors increase topoisomerase II levels and increase cell kill induced by topoisomerase II poisons. We evaluated this hypothesis in a cohort of...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s002800000211

    authors: Dowlati A,Levitan N,Gordon NH,Hoppel CL,Gosky DM,Remick SC,Ingalls ST,Berger SJ,Berger NA

    更新日期:2001-01-01 00:00:00

  • Efficacy and safety of liposome-paclitaxel and carboplatin based concurrent chemoradiotherapy for locally advanced lung squamous cell carcinoma.

    abstract:OBJECTIVE:The aim of this study was to evaluate the efficacy and toxicities of liposome-paclitaxel and carboplatin concurrent with radiotherapy for locally advanced lung squamous cell carcinoma (LSCC). METHODS:The clinical data of 38 patients with locally advanced LSCC treated with liposome-paclitaxel based concurrent...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-018-3640-6

    authors: Chen G,Sheng L,Du X

    更新日期:2018-09-01 00:00:00

  • A phase IB clinical and pharmacokinetic study of the angiogenesis inhibitor SU5416 and paclitaxel in recurrent or metastatic carcinoma of the head and neck.

    abstract:PURPOSE:SU5416 is a novel small organic molecule that non-competitively inhibits the phosphorylation of the VEGF tyrosine kinase receptor, Flk-1. This phase IB study was performed to determine the safety, pharmacokinetics, and preliminary efficacy of the combination of SU5416 and paclitaxel in recurrent or metastatic c...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s00280-004-0871-5

    authors: Cooney MM,Tserng KY,Makar V,McPeak RJ,Ingalls ST,Dowlati A,Overmoyer B,McCrae K,Ksenich P,Lavertu P,Ivy P,Hoppel CL,Remick S

    更新日期:2005-03-01 00:00:00

  • A highly sensitive enzyme-linked immunosorbent assay for etoposide using beta-D-galactosidase as a label.

    abstract::A highly sensitive enzyme-linked immunosorbent assay (ELISA) for etoposide (EP) was developed, which is capable of accurately measuring as little as 40 pg EP/ml. Anti-EP sera were obtained by immunizing rabbits with EP conjugated with mercaptosuccinyl bovine serum albumin (MS.BSA) using N-[beta-(4-diazophenyl)ethyl]ma...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00689094

    authors: Saita T,Fujiwara K,Kitagawa T,Mori M,Takata K

    更新日期:1990-01-01 00:00:00

  • Thymidine enhancement of methotrexate and 5-fluorouracil toxicity in cultured human colon carcinoma.

    abstract::Cultures of human colon carcinoma, HCT-8, were treated with millimolar concentrations of thymidine by different schedules designed to cytokinetically and biochemically modulate methotrexate (MTX) and 5-fluorouracil (FUra) toxicity. Thymidine (dThd)-synchronized HCT-8 cells monitored by flow cytofluorometry showed incr...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00254600

    authors: Benz C,Choti M,Newcomer L,Cadman E

    更新日期:1984-01-01 00:00:00