Circulating vascular endothelial growth factor receptor 2/pAkt-positive cells as a functional pharmacodynamic marker in metastatic colorectal cancers treated with antiangiogenic agent.

abstract：:SHetA2 is a small molecule flexible heteroarotinoid (Flex-Het) with promising cancer prevention and therapeutic activity. Extensive preclinical testing documented lack of SHetA2 toxicity at doses 25 to 150 fold above effective doses. Knowledge of the SHetA2 molecular target(s) that mediate(s) the mechanism of SHetA2 a...

journal_title：Investigational new drugs

authors： Benbrook DM,Nammalwar B,Long A,Matsumoto H,Singh A,Bunce RA,Berlin KD

更新日期：2014-06-01 00:00:00

abstract：:Up to 30% of patients with advanced germ cell tumors will fail induction chemotherapy or will relapse. New agents with activity in this still potentially curable subgroup of patients are needed. Edatrexate (10-ethyl, 10-deaza-aminopterin) is a methotrexate analogue that has preclinical and clinical activity in breast,...

journal_title：Investigational new drugs

authors： Meyers FJ,Lew D,Lara PN Jr,Williamson S,Marshall E,Balcerzak SP,Rivkin SE,Samlowski W,Crawford ED

更新日期：1998-01-01 00:00:00

abstract：:SJG-136 is a synthetic pyrrolobenzodiazepine (PBD) dimer in which two DNA-alkylating subunits are linked through an inert propanedioxy tether. Biophysical and biochemical studies of SJG-136 have shown a remarkable affinity for DNA and potent cytotoxicity in vitro. On this basis, together with its unique sequence selec...

journal_title：Investigational new drugs

authors： Wilkinson GP,Taylor JP,Shnyder S,Cooper P,Howard PW,Thurston DE,Jenkins TC,Loadman PM

更新日期：2004-08-01 00:00:00

abstract：:Echinomycin is a quinoxaline antibiotic that was originally isolated from Streptomyces echinatus. Based on its antitumor activity against two i.p. implanted murine tumors, the B16 melanoma, and the P388 leukemia, it was brought into clinical trials by the National Cancer Institute. Recent studies on its cytotoxic acti...

journal_title：Investigational new drugs

authors： Foster BJ,Clagett-Carr K,Shoemaker DD,Suffness M,Plowman J,Trissel LA,Grieshaber CK,Leyland-Jones B

更新日期：1985-01-01 00:00:00

abstract：:Idarubicin (DMDR), a new analogue of daunorubicin, was administered orally once every 3 weeks at the dose of 40 to 45 mg/m2 to 20 evaluable patients with non-Hodgkin's lymphomas (NHL). Eighty-six percent of patients with favorable histology and 54% with unfavorable histology (intermediate and high grade as IWF) achiev...

journal_title：Investigational new drugs

authors： Lopez M,Di Lauro L,Papaldo P

更新日期：1986-01-01 00:00:00

abstract：:We explored whether barasertib (AZD1152), a selective Aurora B kinase inhibitor, is a substrate for P-glycoprotein (Pgp, MDR1), breast cancer resistance protein (BCRP), and multidrug resistance protein 2 (MRP2) in vitro. Cell survival, drug transport, and competition experiments with barasertib pro-drug and the more a...

journal_title：Investigational new drugs

authors： Marchetti S,Pluim D,van Eijndhoven M,van Tellingen O,Mazzanti R,Beijnen JH,Schellens JH

更新日期：2013-10-01 00:00:00

abstract：PURPOSE:This phase I study aims at assessing the safety and tolerability of LY2603618, a selective inhibitor of Checkpoint Kinase 1, in combination with pemetrexed and determining the maximum tolerable dose and the pharmacokinetic parameters. EXPERIMENTAL DESIGN:This was an open-label, multicenter, dose-escalation stu...

journal_title：Investigational new drugs

authors： Weiss GJ,Donehower RC,Iyengar T,Ramanathan RK,Lewandowski K,Westin E,Hurt K,Hynes SM,Anthony SP,McKane S

更新日期：2013-02-01 00:00:00

abstract：:Twenty-four patients with advanced epidermoid carcinoma of the esophagus were treated with trimetrexate (TMTX), a lipid soluble non-classical antifol. Patients were given TMTX 8 mg/m2 intravenously day 1-5 every 28 days. In nine of these patients the dose was escalated to 12 mg/m2 day 1-5 every 28 days. Three patients...

journal_title：Investigational new drugs

authors： Alberts AS,Falkson G,Badata M,Terblanche AP,Schmid EU

更新日期：1988-12-01 00:00:00

abstract：:Taxol was administered as a 24-hour continuous infusion at 250 mg/m2 in this Phase II trial in patients with adenocarcinomas of the upper gastrointestinal tract (UGIT). Twenty-five patients were entered between July 1991 and June 1992, twenty-three were eligible and were evaluated for toxicity and twenty-two were asse...

journal_title：Investigational new drugs

authors： Einzig AI,Lipsitz S,Wiernik PH,Benson AB 3rd

更新日期：1995-01-01 00:00:00

abstract：:Bryostatin 1 (Bryo) is a naturally occurring macrocyclic lactone with antineoplastic activity. Like the phorbol ester 12-O-tetradecanoyl-phorbol 13-acetate (TPA) it directly activates the calcium- and phospholipid-dependent protein kinase C (PKC), thus generating a number of different cellular responses. We investigat...

journal_title：Investigational new drugs

authors： Steube KG,Grunicke D,Drexler HG

更新日期：1994-01-01 00:00:00

abstract：PURPOSE:To investigate the hypothesis that a systemic agent designed to inhibit dihydropyrimidine dehydrogenase (DPD), the first enzyme in the fluoropyrimidine degradative pathway, could improve the effective amount of 5-fluorouracil (5-FU) delivered to a tumor resulting in enhanced response. PATIENTS AND METHODS:Elig...

journal_title：Investigational new drugs

authors： Leichman CG,Chansky K,Macdonald JS,Doukas MA,Budd GT,Giguere JK,Abbruzzese JL,Southwest Oncology Group.

更新日期：2002-11-01 00:00:00

abstract：:Antiproliferative factor (APF) is a potent frizzled protein 8-related sialoglycopeptide inhibitor of bladder epithelial cell proliferation that mediates its activity by binding to cytoskeletal associated protein 4 in the cell membrane. Synthetic asialylated APF (as-APF) (Galβ1-3GalNAcα-O-TVPAAVVVA) was previously show...

journal_title：Investigational new drugs

authors： Koch KR,Zhang CO,Kaczmarek P,Barchi J Jr,Guo L,Shahjee HM,Keay S

更新日期：2012-10-01 00:00:00

abstract：:Nafazatrom, a synthetic pyrazolinone derivative, has been shown to have substantial antitumor activity in vitro and antitumor and antimetastatic activity in experimental animal systems. The drug has produced no substantial toxicity in preclinical studies and during limited human trials. A phase I clinical trial with t...

journal_title：Investigational new drugs

authors： Hortobagyi GN,Papadoupoulos NE,Frye D,Ajani J,Reuben JM

更新日期：1986-01-01 00:00:00

abstract：PURPOSE:To assess the maximum-tolerated dose (MTD), dose-limiting toxicity (DLT), safety, and tolerability of MN-209, a novel vascular disrupting agent, in patients with advanced solid tumors. STUDY DESIGN:MN-029 was administered weekly for three consecutive weeks out of four; two cycles were planned. Dose escalation ...

journal_title：Investigational new drugs

authors： Traynor AM,Gordon MS,Alberti D,Mendelson DS,Munsey MS,Wilding G,Gammans RE,Read WL

更新日期：2010-08-01 00:00:00

abstract：AIM:5,6-Dimethylxanthenone-4-acetic acid (DMXAA) (ASA404), a low molecular weight antivascular drug currently in clinical trial, acts both directly on the tumour vascular endothelium and indirectly through the induction of inflammatory cytokines and other vasoactive molecules from macrophages and other host cells. We w...

journal_title：Investigational new drugs

authors： Wang LC,Ching LM,Paxton JW,Kestell P,Sutherland R,Zhuang L,Baguley BC

更新日期：2009-06-01 00:00:00

abstract：:This study sought to measure the degree of synergy induced by specific small molecule inhibitors of DNA-PK [NU7026 and IC486241 (ICC)], a major component of the non-homologous end-joining (NHEJ) pathway, with SN38 or oxaliplatin. Synergy between the DNA damaging drugs and the DNA-PK inhibitors was assessed using the s...

journal_title：Investigational new drugs

authors： Davidson D,Coulombe Y,Martinez-Marignac VL,Amrein L,Grenier J,Hodkinson K,Masson JY,Aloyz R,Panasci L

更新日期：2012-06-01 00:00:00

abstract：:CC-1065 is a unique alkylating agent that preferentially binds in the minor groove of double-stranded DNA at adenine-thymine-rich sites. Although it has broad antitumor activity in preclinical models its development was discontinued because of deaths observed during preclinical toxicology studies. Adozelesin is a pote...

journal_title：Investigational new drugs

authors： Foster BJ,LoRusso PM,Poplin E,Zalupski M,Valdivieso M,Wozniak A,Flaherty L,Kasunic DA,Earhart RH,Baker LH

更新日期：1996-01-01 00:00:00

abstract：BACKGROUND:Relatively few studies have examined the activity of alkylating agents in the treatment of advanced colorectal adenocarcinoma. Recent reports have suggested possible therapeutic activity for high-dose intravenous melphalan administered with autologous bone marrow transplantation (BMT) support. We conducted a...

journal_title：Investigational new drugs

authors： Moore DF Jr,Pazdur R,Abbruzzese JL

更新日期：1994-01-01 00:00:00

abstract：OBJECTIVE:Axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, is metabolized primarily by cytochrome P450 (CYP) 3A with minor contributions from CYP1A2, CYP2C19, and glucuronidation. Co-administration with CYP inhibitors may increase systemic expos...

journal_title：Investigational new drugs

authors： Pithavala YK,Tong W,Mount J,Rahavendran SV,Garrett M,Hee B,Selaru P,Sarapa N,Klamerus KJ

更新日期：2012-02-01 00:00:00

abstract：:Infantile hemangioma is the most common vascular tumor of childhood. It is characterized by clinical expansion of endothelial cells and promoted by angiogenic factors. Luteolin is a flavonoid compound that carries anti-cancer and anti-angiogenesis properties. The study aimed to investigate the effect of luteolin in tr...

journal_title：Investigational new drugs

authors： Dai Y,Zheng H,Liu Z,Wang Y,Hu W

更新日期：2021-01-07 00:00:00

abstract：:The effect of the single-chain alkylphospholipid perifosine was analyzed in p53(wild-type) (SKW6.4, OCI and MOLM), p53(mutated) (BJAB, MAVER) and p53(null) (HL-60) leukemic cell lines. Perifosine promoted cytotoxicity with a combination of apoptosis induction in all cell lines and cell cycle block at the G(2)M checkpo...

journal_title：Investigational new drugs

authors： Celeghini C,Voltan R,Rimondi E,Gattei V,Zauli G

更新日期：2011-04-01 00:00:00

abstract：INTRODUCTION:This multicenter, open-label, phase II study was carried out to compare the efficacy and safety of cilengitide (EMD 121974), a selective inhibitor of the cell-surface integrins αVβ3 and αVβ5, with that of docetaxel in patients with advanced non-small-cell lung cancer (NSCLC). METHODS:Patients (n = 140) wi...

journal_title：Investigational new drugs

authors： Manegold C,Vansteenkiste J,Cardenal F,Schuette W,Woll PJ,Ulsperger E,Kerber A,Eckmayr J,von Pawel J

更新日期：2013-02-01 00:00:00

abstract：:Pharmacological intervention to reduce CRC mortality entails the use of oral agents that can avert carcinogenesis. Silibinin, a major component of silymarin isolated from Silybum marianum (L.) was found to possess attractive remedial features. An in vivo study was designed to elucidate the effect of silibinin on the f...

journal_title：Investigational new drugs

authors： Sangeetha N,Aranganathan S,Nalini N

更新日期：2010-06-01 00:00:00

abstract：:Toxicity in the form of marrow suppression has hampered the investigation of intensive chemotherapy as it applies to the treatment of solid tumors. The use of autologous marrow rescue to ameliorate protracted aplasia permits the application of high dose chemotherapy to the treatment of solid tumors. We review the theo...

journal_title：Investigational new drugs

authors： LeMaistre CF,Knight WA 3rd

更新日期：1983-01-01 00:00:00

abstract：:Peloruside A is a microtubule-stabilizing agent that is currently under investigation as a potential anticancer agent. Peloruside A binds to a site on β-tubulin that is distinct to that of the taxanes (paclitaxel and docetaxel) and the epothilones. An attractive clinical quality of microtubule-stabilizing agents is th...

journal_title：Investigational new drugs

authors： Chan A,Singh AJ,Northcote PT,Miller JH

更新日期：2015-06-01 00:00:00

abstract：:Glioblastoma (GBM), one of the most malignant human neoplasias, responds poorly to current treatment modalities, with temozolomide (TMZ) being the drug most frequently used for its treatment. Tetra-O-methyl Nordihydroguaiaretic Acid (M4N) is a global transcriptional repressor of genes dependent on the Sp1 transcriptio...

journal_title：Investigational new drugs

authors： Castro-Gamero AM,Borges KS,Moreno DA,Suazo VK,Fujinami MM,de Paula Gomes Queiroz R,de Oliveira HF,Carlotti CG Jr,Scrideli CA,Tone LG

更新日期：2013-08-01 00:00:00

abstract：:Introduction BTH1677, a 1,3-1,6 beta-glucan immunomodulator, stimulates a coordinated anti-cancer immune response in combination with anti-tumor antibody therapies. This phase II study explored the efficacy, pharmacokinetics (PK), and safety of BTH1677 combined with cetuximab/carboplatin/paclitaxel in untreated stage ...

journal_title：Investigational new drugs

authors： Thomas M,Sadjadian P,Kollmeier J,Lowe J,Mattson P,Trout JR,Gargano M,Patchen ML,Walsh R,Beliveau M,Marier JF,Bose N,Gorden K,Schneller F 3rd

更新日期：2017-06-01 00:00:00

abstract：:The limiting toxicity of low dose continuous infusion 5-fluorouracil (200-300 mg/m2/day) is often palmar-plantar erythrodysesthesia (PPE). PPE developed in 16/25 patients (exact 95% confidence interval of 42%-82%) with metastatic colon cancer enrolled in a phase II trial. In this trial, 5-FU was given continuously at ...

journal_title：Investigational new drugs

authors： Fabian CJ,Molina R,Slavik M,Dahlberg S,Giri S,Stephens R

更新日期：1990-02-01 00:00:00

abstract：:Background AR-67 is a novel camptothecin analogue at early stages of drug development. The phase 1 clinical trial in cancer patients with solid tumors was completed and a population pharmacokinetic model (POP PK) was developed to facilitate further development of this investigational agent. Methods Pharmacokinetic dat...

journal_title：Investigational new drugs

authors： Tang F,Tsakalozou E,Arnold SM,Ng CM,Leggas M

更新日期：2019-12-01 00:00:00

abstract：:Didemnin B is a depsipeptide derived from a Caribbean tunicate (sea squirt) that has demonstrated antineoplastic activity against a variety of murine tumor models, including the L1210 and P388 leukemia, the B16 melanoma, and M5076 sarcoma cell lines. Based on these data, we designed a phase II trial in which 15 patien...

journal_title：Investigational new drugs

authors： Jones DV Jr,Ajani JA,Blackburn R,Daugherty K,Levin B,Patt YZ,Abbruzzese JL

更新日期：1992-08-01 00:00:00