当前位置： SCI文献检索 > CANCER CHEMOTHERAPY AND PHARMACOLOGY期刊下所有文献 > Receptor occupancy theory-based analysis of antiemetic effects and standard doses of 5-HT3 receptor antagonists in cancer patients.

Receptor occupancy theory-based analysis of antiemetic effects and standard doses of 5-HT3 receptor antagonists in cancer patients.

Abstract：

PURPOSE:The aim of this study was to determine the usefulness of receptor occupancy theory-based analysis using pharmacokinetic and pharmacodynamic parameters for predicting the average receptor occupancy (PhiB) in humans of each of five 5-HT3 antagonists administered at standard doses. METHODS:The relationship between the PhiB value and the complete vomiting inhibition rate after a single intravenous administration of cisplatin (not less than 50 mg/m2) was analyzed. RESULTS:The predicted PhiB values after intravenous administration and oral administration of 5-HT3 antagonists were more than 65% and 50%, respectively, suggesting that relatively high receptor occupancy is required to elicit sufficient antiemetic effects of 5-HT3 antagonists. Moreover, significant ( P<0.05) linear relationships were found between PhiB values and complete vomiting inhibition rates of 5-HT3 antagonists in preventive cisplatin therapy, with correlation coefficients higher than 0.9, suggesting that the 5-HT3 receptor occupancy is an appropriate index of clinical efficacy of 5-HT3 antagonists, with higher receptor occupancy indicating more extensive antiemetic action. CONCLUSION:The receptor occupancy theory-based analysis of the antiemetic effect of a 5-HT3 receptor antagonist used in this study should be very useful for not only estimating a rational dosage regimen but also determining the standard dose of a new drug using experimental data obtained in a preclinical study.

journal_name

Cancer Chemother Pharmacol

journal_title

Cancer chemotherapy and pharmacology

authors

Yamada Y,Sugiura M,Higo K,Ozeki T,Takayanagi R,Okuyama K,Yamamoto K,Satoh H,Sawada Y,Iga T

doi

10.1007/s00280-004-0798-x

keywords:

subject

Has Abstract

pub_date

2004-08-01 00:00:00

pages

185-90

issue

2

eissn

0344-5704

issn

1432-0843

journal_volume

54

pub_type

杂志文章

相关文献

CANCER CHEMOTHERAPY AND PHARMACOLOGY文献大全
  • Pharmacodynamic modeling of prolonged administration of etoposide.

    abstract：PURPOSE:A refined pharmacodynamic model for toxicity is necessary for successful adaptive control of the administration of an anticancer drug to avoid toxicity. We sought to establish a pharmacodynamic model of leukopenia in a 14-day administration of etoposide. METHODS:Pharmacokinetic data of 32 patients treated with...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 临床试验,杂志文章

    doi：10.1007/s002800050538

    authors： Minami H,Ratain MJ,Ando Y,Shimokata K

    更新日期：1996-01-01 00:00:00

  • A phase II study of human rDNA alpha-2 interferon in patients with low grade non-Hodgkin's lymphoma.

    abstract：:Thirty-five patients with a diagnosis of non-Hodgkin's lymphoma of low histological grade were treated with 2 X 10(6)/m2 of human rDNA alpha 2 IFN-a2 by subcutaneous injection. Treatment was continued until progressive disease was documented or one year of therapy had been given. None of the patients had to stop treat...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00253065

    authors： Wagstaff J,Loynds P,Crowther D

    更新日期：1986-01-01 00:00:00

  • Comparative brain and plasma pharmacokinetics and anticancer activities of chlorambucil and melphalan in the rat.

    abstract：:Equimolar doses of chlorambucil and melphalan (both 10 mg/kg) were administered i.v. to anesthetized rats, and the plasma and brain concentrations of chlorambucil, its metabolites 3,4-dehydrochlorambucil and phenylacetic mustard, and melphalan were determined by high-performance liquid chromatography from 5 to 240 min...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00262729

    authors： Greig NH,Sweeney DJ,Rapoport SI

    更新日期：1988-01-01 00:00:00

  • A pharmacodynamic model of Bcr-Abl signalling in chronic myeloid leukaemia.

    abstract：:Chronic myeloid leukaemia (CML) is an unusual malignancy in which myeloid progenitor cells are transformed by a single chromosomal translocation where the Bcr domain of chromosome 22 is placed adjacent to the proto-oncogene c-Abl of chromosome 9, resulting in constitutive Abl tyrosine kinase activity. This has a twofo...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-014-2556-z

    authors： Jackson RC,Radivoyevitch T

    更新日期：2014-10-01 00:00:00

  • Experimental study of the inhibition of human hepatocarcinoma Bel7402 cells by the tripeptide tyroserleutide(YSL).

    abstract：PURPOSE:To investigate the antitumor effects of tyroserleutide (tyrosyl-seryl-leucine, YSL) on human Bel7402 hepatocarcinoma in vitro and in vivo, with preliminary exploration of its antitumor mechanism. METHODS:MTT was used to observe the anticarcinogenic effects of YSL on human hepatocarcinoma Bel7402 cells in vitro...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-005-0046-z

    authors： Lu R,Jia J,Bao L,Fu Z,Li G,Wang S,Wang Z,Jin M,Gao W,Yao Z

    更新日期：2006-01-01 00:00:00

  • Cetuximab plus pemetrexed as second-line therapy for fluorouracil-based pre-treated metastatic esophageal squamous cell carcinoma.

    abstract：PURPOSE:The aim of this study was to evaluate the efficacy and toxicity of cetuximab and pemetrexed as the second-line treatment for advanced esophageal cancer patients, who had undergone treatment with the standard cisplatin and 5-FU regimens. METHODS:A total of 29 patients accepted this treatment. Cetuximab was admi...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 临床试验,杂志文章

    doi：10.1007/s00280-015-2854-0

    authors： Tian J,Shang M,Shi SB,Han Y,Xu J

    更新日期：2015-10-01 00:00:00

  • Antitumor alkylating agents: in vitro cross-resistance and collateral sensitivity studies.

    abstract：:Cell lines resistant to five antitumor alkylating agents (CDDP, PAM, 4-HC, HN2, and BCNU) were developed from five parental human tumor lines representative of solid tumors with a range of sensitivities to antitumor alkylating agents. The parental cell lines were SCC-25 squamous carcinoma of the head and neck, MCF-7 b...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00685328

    authors： Frei E 3rd,Holden SA,Gonin R,Waxman DJ,Teicher BA

    更新日期：1993-01-01 00:00:00

  • Lack of strain-related differences in drug metabolism and efflux transporter characteristics between CD-1 and athymic nude mice.

    abstract：:CD-1 mice are commonly used in oncology metabolism and toxicity to support drug discovery and development and to examine drug metabolism and toxicity properties of new chemical entities. On the other hand, athymic nude mice are the preferred animals to investigate tumor growth inhibition. Therefore, a frequently asked...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-004-0898-7

    authors： Martignoni M,de Kanter R,Moscone A,Grossi P,Monshouwer M

    更新日期：2005-02-01 00:00:00

  • Comparison of the potency of glycosylated and nonglycosylated recombinant human granulocyte colony-stimulating factors in neutropenic and nonneutropenic CD rats.

    abstract：:Recent studies in human bone-marrow culture and healthy human volunteers suggest that lenograstim [glycosylated, recombinant human granulocyte colony-stimulating factor (rHuG-CSF) produced in Chinese hamster ovary (CHO) cells] has greater in vivo potency than filgrastim [nonglycosylated, methionine-extended recombinan...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s002800050570

    authors： Nohynek GJ,Plard JP,Wells MY,Zerial A,Roquet F

    更新日期：1997-01-01 00:00:00

  • Preclinical pharmacokinetics and in vitro metabolism of brivanib (BMS-540215), a potent VEGFR2 inhibitor and its alanine ester prodrug brivanib alaninate.

    abstract：PURPOSE:Brivanib alaninate is a prodrug of brivanib (BMS-540215), a potent oral VEGFR-2 inhibitor and is currently in development for the treatment of hepatocellular and colon carcinomas. In vitro and in vivo studies were conducted to characterize the preclinical pharmacokinetics and disposition of brivanib and brivani...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-009-1002-0

    authors： Marathe PH,Kamath AV,Zhang Y,D'Arienzo C,Bhide R,Fargnoli J

    更新日期：2009-12-01 00:00:00

  • Immunosuppressant inhibition of P-glycoprotein function is independent of drug-induced suppression of peptide-prolyl isomerase and calcineurin activity.

    abstract：PURPOSE:P-glycoprotein is a 170-kDa plasma membrane multidrug transporter that actively exports cytotoxic substances from cells. Overexpression of P-glycoprotein by tumor cells is associated with a multidrug-resistant phenotype. Immunosuppressive agents such as cyclosporins and macrolides, have been shown to attenuate ...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s002800050960

    authors： Mealey KL,Barhoumi R,Burghardt RC,McIntyre BS,Sylvester PW,Hosick HL,Kochevar DT

    更新日期：1999-01-01 00:00:00

  • FSTL1 increases cisplatin sensitivity in epithelial ovarian cancer cells by inhibition of NF-κB pathway.

    abstract：OBJECTIVE:To investigate the effects of FSTL1-mediated NF-κB signaling pathway on cisplatin (DDP) sensitivity of EOC cells. METHODS:FSTL1 expression was determined in epithelial ovarian cancer (EOC) tissues and corresponding adjacent tissues using immunohistochemistry. SKOV3 and SKOV3/DDP cells were transfected and gr...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-020-04215-9

    authors： Liu YK,Jia YJ,Liu SH,Ma J

    更新日期：2021-01-03 00:00:00

  • Hemodialysis does not impact axitinib exposure: clinical case of a patient with metastatic renal cell carcinoma.

    abstract：:Axitinib is approved with indication in patients with advanced renal cell carcinoma (RCC). Due to the localization of this cancer, physicians sometimes have to deal with hemodialyzed patients. Data exploring hemodialysis (HD) impact on axitinib pharmacokinetic (PK) or safety are lacking. To date, no data have been pub...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-017-3320-y

    authors： Thiery-Vuillemin A,Orillard E,Mouillet G,Calcagno F,Devillard N,Bouchet S,Royer B

    更新日期：2017-06-01 00:00:00

  • The role of methoxymorpholino anthracycline and cyanomorpholino anthracycline in a sensitive small-cell lung-cancer cell line and its multidrug-resistant but P-glycoprotein-negative and cisplatin-resistant counterparts.

    abstract：:The cytotoxic action of two morpholino anthracyclines, methoxymorpholino anthracycline (MRA-MT, FCE 23,762) and cyanomorpholino anthracycline (MRA-CN), was compared with the cytotoxicity of doxorubicin (DOX), the topoisomerase II inhibitor etoposide (VP-16), the topoisomerase I inhibitor camptothecin, methotrexate, an...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00689457

    authors： van der Graaf WT,Mulder NH,Meijer C,de Vries EG

    更新日期：1995-01-01 00:00:00

  • Intravenous paclitaxel against metastasis of human gastric tumors of diffuse type.

    abstract：PURPOSE:Gastric cancer is one of the leading cancerous diseases worldwide. It is diagnosed often at the advanced stage for which chemotherapy is the main treatment option. The prognosis remains poor for metastatic, especially the diffuse type, gastric cancers. We investigated the efficacy of intravenously administered ...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-009-1222-3

    authors： Tuan TF,Tsai ML,Yeh KC,Huang HC,Chung CT,Huang CL,Han CH,Chen CP,Wang MH,Shen CC,Lai YK,Lee WS,Hwang LL,Chen CT

    更新日期：2010-09-01 00:00:00

  • Exposure-response relationship for ramucirumab from the randomized, double-blind, phase 3 REVEL trial (docetaxel versus docetaxel plus ramucirumab) in second-line treatment of metastatic non-small cell lung cancer.

    abstract：PURPOSE:Ramucirumab plus docetaxel improved survival in REVEL, a randomized phase 3 trial for patients with Stage IV non-small cell lung cancer after standard platinum-based chemotherapy. This exploratory analysis evaluated the exposure-response relationship of ramucirumab from REVEL. METHODS:Patients received ramucir...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章,随机对照试验

    doi：10.1007/s00280-018-3560-5

    authors： Smit EF,Garon EB,Reck M,Cappuzzo F,Bidoli P,Cohen RB,Gao L,O'Brien LM,Lee P,Zimmermann A,Ferry DR,Melemed AS,Pérol M

    更新日期：2018-07-01 00:00:00

  • Effects of gemcitabine on cell proliferation and apoptosis in non-small-cell lung cancer (NSCLC) cell lines.

    abstract：:We evaluated the antiproliferative and the proapoptotic ability of gemcitabine in three non-small-cell lung cancer (NSCLC) cell lines. NCI-H292 (mucoepidermoid carcinoma), NCI-CorL23 (large-cell carcinoma) and NCI-Colo699 (adenocarcinoma) cells were cultured with and without 0.5, 0.05 and 0.005 microM gemcitabine for ...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s002800000183

    authors： Pace E,Melis M,Siena L,Bucchieri F,Vignola AM,Profita M,Gjomarkaj M,Bonsignore G

    更新日期：2000-01-01 00:00:00

  • Dosing sequence-dependent pharmacokinetic interaction of oxaliplatin with paclitaxel in the rat.

    abstract：BACKGROUND:In a phase I clinical trial of oxaliplatin (OPT) in combination with paclitaxel (PXL), a pharmacokinetic interaction was observed when OPT was given as a 2-h i.v. infusion followed by a 1-h i.v. infusion of PXL. The purpose of this study was to use a rat model to evaluate whether the pharmacokinetic interact...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-002-0531-6

    authors： Liu J,Kraut EH,Balcerzak S,Grever M,D'Ambrosio S,Chan KK

    更新日期：2002-12-01 00:00:00

  • Uncoupling protein downregulation in doxorubicin-induced heart failure improves mitochondrial coupling but increases reactive oxygen species generation.

    abstract：PURPOSE:Doxorubicin-based chemotherapy is limited by the development of dose-dependent left ventricular dysfunction and congestive heart failure caused by reactive oxygen species (ROS). Uncoupling proteins (UCP) can inhibit mitochondrial ROS production as well as decrease myocyte damage from exogenous ROS. Prior studie...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-010-1441-7

    authors： Bugger H,Guzman C,Zechner C,Palmeri M,Russell KS,Russell RR 3rd

    更新日期：2011-06-01 00:00:00

  • Prognosis after hepatic resection in patients with hepatocellular carcinoma, estimated on the basis of the morphometric indices.

    abstract：:To determine whether the morphometric indices of hepatocellular carcinoma (HCC) correlated with the prognoses, the microscopic morphometric values for 84 HCC cases treated by hepatic resection were studied using an image analyzer in relation to the survival rate and the gross classification. The mean survival time (MS...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00686663

    authors： Kawai Y,Takeshige K,Nunome M,Kuroda H,Suzuki H,Banno K,Koide T,Kobayashi H,Owa Y,Koike A

    更新日期：1994-01-01 00:00:00

  • A phase I study of HER1, HER2 dual kinase inhibitor lapatinib plus the proteasome inhibitor bortezomib in patients with advanced malignancies.

    abstract：PURPOSE:This phase I trial evaluated the maximum tolerated dose, safety and preliminary efficacy of lapatinib, a HER1, HER2 dual kinase inhibitor plus bortezomib, a proteasome inhibitor, in adult patients with advanced malignancies. METHODS:Patients were enrolled in a standard 3 + 3 design with lapatinib (L) 750, 1000...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-019-03947-7

    authors： Lynce F,Wang H,Petricoin EF,Pohlmann PR,Smaglo B,Hwang J,He AR,Subramaniam DS,Deeken J,Marshall J,Pishvaian MJ

    更新日期：2019-11-01 00:00:00

  • A pharmacodynamically guided dose selection of PF-00337210 in a phase I study in patients with advanced solid tumors.

    abstract：PURPOSE:PF-00337210 is an oral, highly selective vascular endothelial growth factor receptor (VEGFR) inhibitor. We evaluated a composite of biomarkers in real time to identify the recommended phase 2 dose (RP2D) and preliminary anticancer activity of PF-00337210. PATIENTS AND METHODS:Patients (Pts) with advanced cance...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-016-2958-1

    authors： Bruce JY,LoRusso PM,Goncalves PH,Heath EI,Sadowski E,Shalinsky DR,Zhang Y,Traynor AM,Breazna A,Ricart AD,Tortorici M,Liu G

    更新日期：2016-03-01 00:00:00

  • Tumor inhibition by titanocene complexes: influence on xenografted human adenocarcinomas of the gastrointestinal tract.

    abstract：:The present study deals with the influence of some bis(eta 5-cyclopentadienyl)titanium(IV) (titanocene) complexes, mainly represented by titanocene dichloride, on the development of several human gastrointestinal (GI) carcinomas (one stomach, seven colon, four sigmoid, and two rectal adenocarcinomas), all xenografted ...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00451646

    authors： Köpf-Maier P

    更新日期：1989-01-01 00:00:00

  • The bioavailability of oral intermediate-dose methotrexate. Effect of dose subdivision, formulation, and timing in the chemotherapy cycle.

    abstract：:The oral bioavailability of methotrexate is variable and may be dose-dependent. The absorption of 'interval' oral methotrexate, which is given between cycles of chemotherapy, is unknown. The bioavailability of oral methotrexate has been studied in eight patients, acting as their own controls, to assess the effect of s...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00257121

    authors： Harvey VJ,Slevin ML,Woollard RC,Johnston A,Barnett MJ,Wrigley PF,Turner P

    更新日期：1984-01-01 00:00:00

  • Epipodophyllotoxin (VP16-213) in small cell carcinoma of the Bronchus resistant to initial combination chemotherapy.

    abstract：:Thirty-eight patients with small cell carcinoma of the bronchus resistant to initial chemotherapy with cyclophosphamide methotrexate and CCNU, were treated with VP16-213 alone in a dose of 120 mg/m2 i.v. on days 1, 3, and 5 every 3 weeks. Twelve patients died before three courses of treatment. In 26 patients who recei...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00254544

    authors： Harper PG,Dally MB,Geddes DM,Spiro SG,Smyth JF,Souhami RL

    更新日期：1982-01-01 00:00:00

  • Tumor-tissue and plasma concentrations of platinum during chemotherapy of non-small-cell lung cancer patients.

    abstract：:Tumor-tissue and plasma concentrations of platinum were studied prospectively in two groups of eight patients who were suffering from advanced non-small-cell lung cancer. Treatments including two different schedules of cisplatin administration (25 vs 100 mg/m2 on day 1) were compared. At 30 min after the beginning of ...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00689280

    authors： Pujol JL,Cupissol D,Gestin-Boyer C,Bres J,Serrou B,Michel FB

    更新日期：1990-01-01 00:00:00

  • Lenalidomide: in vitro evaluation of the metabolism and assessment of cytochrome P450 inhibition and induction.

    abstract：PURPOSE:To assess the potential for drug-drug interactions between lenalidomide and substrates and inhibitors of cytochrome P450 (CYP) isozymes. METHODS:In vitro metabolism of lenalidomide by human liver microsomes, recombinant human CYPs and human hepatocytes was evaluated. The inhibitory and inductive effects of len...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-008-0867-7

    authors： Kumar G,Lau H,Laskin O

    更新日期：2009-05-01 00:00:00

  • Reduced activity of topoisomerase II in an Adriamycin-resistant human stomach-adenocarcinoma cell line.

    abstract：:A human stomach-adenocarcinoma cell line (MKN-45) was selected for resistance to Adriamycin by stepwise exposure to increasing concentrations of this agent. The resulting cell line (MKN/ADR) exhibited a high level of cross-resistance to topoisomerase II (topo II)-targeted drugs such as Adriamycin, mitoxantrone, and et...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s002800050751

    authors： Son YS,Suh JM,Ahn SH,Kim JC,Yi JY,Hur KC,Hong WS,Muller MT,Chung IK

    更新日期：1998-01-01 00:00:00

  • Enhancing the activity of platinum-based drugs by improved inhibitors of ERCC1-XPF-mediated DNA repair.

    abstract：PURPOSE:The ERCC1-XPF 5'-3' DNA endonuclease complex is involved in the nucleotide excision repair pathway and in the DNA inter-strand crosslink repair pathway, two key mechanisms modulating the activity of chemotherapeutic alkylating agents in cancer cells. Inhibitors of the interaction between ERCC1 and XPF can be us...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/s00280-020-04213-x

    authors： Ciniero G,Elmenoufy AH,Gentile F,Weinfeld M,Deriu MA,West FG,Tuszynski JA,Dumontet C,Cros-Perrial E,Jordheim LP

    更新日期：2021-01-05 00:00:00

  • Successful treatment of a patient with acute nonlymphoblastic leukemia (ANLL) and anthracycline cardiomyopathy with 4' (9-acridinylamino) methanesulfon-m-anisidide (AMSA).

    abstract：:A patient with acute nonlymphoblastic leukemia in relapse and anthracycline cardiomyopathy was treated with AMSA in combination with cytosine arabinoside and thioguanine (AAT). Induction of remission was accomplished after one course of therapy without development of congestive heart failure. Radionuclide studies done...

    journal_title：Cancer chemotherapy and pharmacology

    pub_type： 杂志文章

    doi：10.1007/BF00257232

    authors： Fanucchi MP,Arlin ZA

    更新日期：1982-12-01 00:00:00