Abstract：
PURPOSE:Ridaforolimus, a potent inhibitor of the mammalian target of rapamycin (mTOR), is under development for the treatment for solid tumors. This open-label, randomized, 3-period crossover study investigated the effect of food on the pharmacokinetics of ridaforolimus 40 mg as well as safety and tolerability of the study medication. METHODS:Ridaforolimus was administered to 18 healthy, male subjects (mean age 36.4 years) in the fasted state, following ingestion of a light breakfast, and following a high-fat breakfast. Whole blood samples were collected from each subject pre-dose and 1, 2, 3, 4, 6, 8, 24, 48, 72, 96, and 168 h post-dose. RESULTS:The geometric mean (95 % confidence interval, CI) fasted blood area under the curve (AUC(0-∞)) and maximum concentration (C(max)) were 1940 (1510, 2500) ng h/mL and 116 (87, 156) ng/mL, respectively, and median time to C(max) (T(max)) and average apparent terminal half-life (t(1/2)) were 6.0 and 64.5 h, respectively. Both T(max) and t(1/2) were similar in the fasted and fed states. With a light breakfast, the geometric mean intra-individual ratios (GMRs) for AUC(0-∞) and C(max) (fed/fasted) and 90 % CIs were 1.06 (0.85, 1.32) and 1.15 (0.83, 1.60); following a high-fat breakfast, the AUC(0-∞) and C(max) GMRs (90 % CI) were 1.46 (1.18, 1.81) and 1.12 (0.81, 1.53), respectively. CONCLUSIONS:Increases in ridaforolimus exposure following both the light and high-fat breakfasts were not considered to be clinically meaningful. Ridaforolimus was generally well tolerated, and there were no discontinuations due to drug-related AEs. Ridaforolimus should be given without regard to food.
journal_name
Cancer Chemother Pharmacoljournal_title
Cancer chemotherapy and pharmacologyauthors
Stroh M,Li X,Marsilio S,Panebianco D,Johnson-Levonas A,Juan A,Orford K,Agrawal N,Trucksis M,Wagner JA,Murphy G,Iwamoto Mdoi
10.1007/s00280-012-1897-8subject
Has Abstractpub_date
2012-07-01 00:00:00pages
177-82issue
1eissn
0344-5704issn
1432-0843journal_volume
70pub_type
杂志文章,随机对照试验abstract：:DDMP, a diaminopyrimidine folate antagonist, was given to 26 tumor patients in a dosage of 50 mg/m2 per week orally, simultaneously with 3 mg CF i.m. or i.v. The CF dose was increased to 30 mg in patients showing evidence of toxicity, and withdrawn in the absence of toxicity. The dose-limiting toxicity was seen in mye...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00254043
更新日期：1978-01-01 00:00:00
abstract：PURPOSE:It has recently been recognised that anticancer chemotherapy can elicit an immunogenic form of apoptosis characterised by the exposure of calreticulin (CRT) on the surface of dying tumour cells, entailing an immune response that contributes to the therapeutic outcome. CRT exposure has been found to be induced b...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s00280-010-1302-4
更新日期：2010-08-01 00:00:00
abstract：PURPOSE:Oxaliplatin and satraplatin demonstrate activity against cisplatin-resistant tumor cells. Although the two platinum analogs are structurally-related, oxaliplatin is more active. Therefore, studies focusing on protein expression profiling were undertaken to identify the molecular mechanism for the difference in ...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s00280-020-04085-1
更新日期：2020-06-01 00:00:00
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
更新日期：1982-12-01 00:00:00
abstract：:To determine whether dimethylsulfoxide (DMSO) can potentiate antitumor activity of cyclophosphamide (CYC) in patients with squamous cell carcinoma of the lung, 14 patients were treated with 5 l of a 5% or 6% DMSO solution PO over 3 days and 1,500 mg CYC/m2 IV as a 60-min infusion on the third day of treatment. Serial ...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00262327
更新日期：1981-01-01 00:00:00
abstract：:The purpose of this study was to evaluate the response rate, methotrexate plasma levels, and toxicity of a three-drug regimen in patients with gastric carcinoma. A total of 37 patients with advanced measurable adenocarcinoma of the stomach were treated with Adriamycin, methotrexate, and 5-fluorouracil (AMF). Adriamyci...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00254103
更新日期：1989-01-01 00:00:00
abstract：:The metabolic disposition and pharmacokinetics of TNP-470 were investigated in rhesus monkeys following intravenous administration of 5 mg/kg of [3H]-TNP-470. Rapid and extensive metabolism of parent drug to six metabolites occurred as demonstrated by the absence of unchanged drug in plasma and urine at time points as...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s002800050458
更新日期：1996-01-01 00:00:00
abstract：:Colchicine is secreted into bile as a major pathway of elimination. Cyclosporine (CsA) inhibits colchicine biliary secretion. In the present study, the effects of cyclosporine and its vehicle (cremophor) on the partitioning of colchicine across the liver were studied. CsA decreased the colchicine bile/plasma ratio fro...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00685886
更新日期：1993-01-01 00:00:00
abstract：PURPOSE:To assess the activity and safety of combined folinic acid (FA), 5-fluorouracil (5-FU) and mitomycin C (MMC) in metastatic breast cancer patients previously treated with at least two chemotherapy regimens. PATIENTS AND METHODS:A total of 104 consecutive patients were enrolled for treatment with FA 100 mg/m(2) ...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s00280-002-0495-6
更新日期：2002-10-01 00:00:00
abstract：PURPOSE:The purpose of this study was to evaluate the expression of ser-miRNAs at different periods during treatment and analyze their relationship with therapeutic response and prognosis in HER2-positive breast cancer patients receiving neoadjuvant chemotherapy combined with trastuzumab (NCCT). METHODS:Venous blood w...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s00280-019-03937-9
更新日期：2019-11-01 00:00:00
abstract：:Previous studies have demonstrated that treatment with fludarabine 4 h prior to arabinosylcytosine (ara-C) potentiates the accumulation of the active triphosphate of ara-C (ara-CTP) in leukemic lymphocytes. The clinical efficacy of this combination was evaluated in 15 patients with chronic lymphocytic leukemia (CLL) t...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00686108
更新日期：1994-01-01 00:00:00
abstract：:To test the feasibility of a regimen of high-dose cisplatin, ifosfamide, and etoposide (VP-16; VIPP regimen), we registered 15 patients with advanced non-small-cell lung cancer in a phase I trial of the Northern California Oncology Group. One cycle of treatment consisted of high-dose cisplatin given at 100 mg/m2 i.v. ...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00686041
更新日期：1994-01-01 00:00:00
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
更新日期：1989-01-01 00:00:00
abstract：:The local therapeutic effects and 5-year survival rates obtained following subsegmental transcatheter arterial embolization (TAE) therapy for small hepatocellular carcinomas (HCCs) were retrospectively analyzed. A total of 124 nodular-type HCC lesions measuring less than 4 cm in diameter in 100 patients with liver cir...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00686674
更新日期：1994-01-01 00:00:00
abstract：:MKT-077 (1-ethyl-2-[[3-ethyl-5-(3-methylbenzothiazolin-2-yliden)]-4- oxothiazolidin-2-ylidenemethyl] pyridinium chloride), a novel rhodacyanine dye in phase I/II clinical trials, may provide a new approach to cancer therapy based on the accumulation in the mitochondria of the cells of certain carcinomas, for example, ...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s002800050898
更新日期：1999-01-01 00:00:00
abstract：:The dextromethorphan-O-demethylase activity determined in human liver microsomes was used to screen various anticancer drugs for their ability to inhibit this cytochrome CYP2D6-dependent activity. Competitive inhibition indicates that the drug binds the enzyme and is potentially subjected to a polymorphic metabolism. ...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00685896
更新日期：1993-01-01 00:00:00
abstract：PURPOSE:Our previous studies have reported the antitumor effect of oleandrin on osteosarcoma; however, its chemosensitizing effect in osteosarcoma treatment is still unknown. Therefore, we explored the sensitizing effects of oleandrin to cisplatin in osteosarcoma and investigated the potential mechanisms. METHODS:Afte...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s00280-018-3692-7
更新日期：2018-12-01 00:00:00
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
更新日期：1999-01-01 00:00:00
abstract：:Nine children with poor-prognosis malignancies--seven with advanced neuroblastoma and two with metastatic Ewing's sarcoma--were given high doses of melphalan (HDM), 150 mg/m2 (3 patients) and 180 mg/m2 (6 patients), as a 'late intensification' agent combined with noncryopreserved autologous bone marrow transplants. Me...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00263898
更新日期：1985-01-01 00:00:00
abstract：PURPOSE:This study evaluated the maximum tolerated dose (MTD) and the dose limiting toxicity (DLT) of erlotinib when combined to irinotecan and capecitabine in pre-treated metastatic colorectal cancer patients. METHODS:Five dose level combinations with irinotecan (from 180 to 240 mg/m(2), day 1, q21), capecitabine (1,...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s00280-008-0852-1
更新日期：2009-06-01 00:00:00
abstract：INTRODUCTION:Limited information on second-line treatment in patients with pancreatic adenocarcinoma is available. At time of first-line treatment failure, approximately half of the patients are candidates for further treatment. MATERIAL AND METHODS:A retrospective review of 183 patients submitted to second-line thera...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章,多中心研究
doi：10.1007/s00280-007-0653-y
更新日期：2008-09-01 00:00:00
abstract：:Thirty-three patients with advanced transitional cell carcinoma of the urinary tract (23 bladder cases, 8 ureter cases, and 2 renal pelvis cases) were treated by three-drug combination chemotherapy using two protocols (protocol I: Adriamycin 50 mg/m2, cyclophosphamide 500 mg/m2, and 5-fluorouracil 500 mg/m2, protocol ...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00256716
更新日期：1983-01-01 00:00:00
abstract：PURPOSE:Ibrutinib is an orally administered, irreversible Bruton's tyrosine kinase inhibitor for treatment of B-cell malignancy. This study evaluated the effects of single-dose ibrutinib at therapeutic and supratherapeutic exposures on cardiac repolarization in healthy subjects. METHODS:Part 1 used an open-label, two-...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s00280-017-3471-x
更新日期：2017-12-01 00:00:00
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
更新日期：1994-01-01 00:00:00
abstract：:To evaluate the value of beta-2-microglobulin as an indicator of acute and long-term cis-platinum-induced nephrotoxicity, 51Cr-EDTA clearance and serum concentration and urinary excretion of beta-2-microglobulin were measured in 18 patients treated with a regimen including cis-platinum. Before treatment all values wer...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00258126
更新日期：1985-01-01 00:00:00
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
更新日期：2009-03-01 00:00:00
abstract：PURPOSE:A metronomic schedule of chemotherapy (resulting in a greater frequency of drug delivery) has shown efficacy in head and neck cancer. Our aim was to investigate the overall survival in tongue cancer patients with metronomic neoadjuvant chemotherapy with bleomycin compared to those with surgery alone. METHODS:I...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s00280-016-3141-4
更新日期：2016-10-01 00:00:00
abstract：PURPOSE:Fenretinide is a synthetic retinoid with activity in prostate cancer and other cell lines. The aim of this study was to assess the efficacy and tolerability of fenretinide in chemotherapy-naïve men with hormone refractory prostate cancer. METHODS:Eligibility criteria included hormone refractory prostate cancer...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章,多中心研究
doi：10.1007/s00280-009-1228-x
更新日期：2010-10-01 00:00:00
abstract：:The antimetabolite 1-beta-D-arabinofuranosyl-cytosine (ara-C) has proven to be one of the most effective agents available for the treatment of acute leukemia. While ara-C has been implicated as a potent inhibitor of mammalian cell DNA replication, the specific mechanism by which ara-C kills cells is not known. In this...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/s002800050496
更新日期：1996-01-01 00:00:00
abstract：:The pharmakokinetic profiles of intraperitoneally infused platinum analogues were determined in 13 women exhibiting minimal residual disease following surgery and systemic chemotherapy for epithelial ovarian cancer or fallopian tube carcinoma by following the disposition of tracer doses of 195mPt radiolabel. Six patie...
journal_title：Cancer chemotherapy and pharmacology
pub_type： 杂志文章
doi：10.1007/BF00685543
更新日期：1991-01-01 00:00:00
