INNO-206, the (6-maleimidocaproyl hydrazone derivative of doxorubicin), shows superior antitumor efficacy compared to doxorubicin in different tumor xenograft models and in an orthotopic pancreas carcinoma model.

abstract：:We have previously described a human pancreatic-ribonuclease variant, named PE5, which carries a non-contiguous extended bipartite nuclear localization signal. This signal comprises residues from at least three regions of the protein. We postulated that the introduction of this signal in the ribonuclease provides it w...

journal_title：Investigational new drugs

authors： Tubert P,Rodríguez M,Ribó M,Benito A,Vilanova M

更新日期：2011-10-01 00:00:00

abstract：:Estrogens play a central role in reproductive physiology. The cellular effects of estrogens are mediated by binding to nuclear receptors (ER) which activate transcription of genes involved in cellular growth control. At least two such receptors, designated ERalpha and ERbeta, mediate these effects in conjunction with ...

journal_title：Investigational new drugs

authors： Dhingra K

更新日期：1999-01-01 00:00:00

abstract：OBJECTIVE:The anti-vascular endothelial growth factor (VEGF) antibody bevacizumab has received considerable attention as a first-line treatment of advanced colorectal cancers. Difficulties associated with effectively monitoring the activity of this drug have prompted us to seek a pharmacodynamic marker suitable for def...

journal_title：Investigational new drugs

authors： Shin SJ,Hwang JW,Ahn JB,Rha SY,Roh JK,Chung HC

更新日期：2013-02-01 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：:Cancer is one of the major causes of death for non-transmissible chronic diseases worldwide. Conventional treatments including surgery, chemotherapy and external beam radiotherapy are generally far from curative. Complementary therapies are attempted for achieving more successful treatment response. Systemic targeted ...

journal_title：Investigational new drugs

authors： Cona MM,Wang H,Li J,Feng Y,Chen F,de Witte P,Verbruggen A,Ni Y

更新日期：2012-10-01 00:00:00

abstract：PURPOSE:To evaluate the response to oral Etoposide when combined with mesna, ifosfamide, and mitoxantrone in patients with relapsed and/or refractory lymphoma. To evaluate response and its duration after administration of intravenous Etoposide, methylprednisolone, high-dose cytosine arabinoside, and cisplatin (ESHAP) a...

journal_title：Investigational new drugs

authors： Romaguera JE,Rodriguez MA,Hagemeister FB,McLaughlin P,Swan F,Moore DF Jr,Sarris AH,Younes A,Hill D,Cabanillas F

更新日期：1994-01-01 00:00:00

abstract：:Withaferin A (WA), a steroidal lactone derived from the plant Vassobia breviflora, has been reported to have anti-proliferative, pro-apoptotic, and anti-angiogenic properties against cancer growth. In this study, we identified several key underlying mechanisms of anticancer action of WA in glioblastoma cells. WA was f...

journal_title：Investigational new drugs

authors： Grogan PT,Sleder KD,Samadi AK,Zhang H,Timmermann BN,Cohen MS

更新日期：2013-06-01 00:00:00

abstract：:In this study, 30 evaluable patients with advanced carcinoma of the breast were treated with cyclophosphamide 600 mg/m2 i.v. followed one day later with mitoxantrone (Novantrone; dihydroxyanthracenedione) 16 mg/m2 i.v. Drug treatment was repeated every 3-4 weeks, for a maximum of 12 cycles. The overall response rate w...

journal_title：Investigational new drugs

authors： Periti P,della Cuna GR,Pannuti F,Mazzei T,Preti P,Martoni A,Mini E

更新日期：1985-01-01 00:00:00

abstract：:To explore the clinical significance of the level of HER2/neu gene amplification in a homogenous cohort of 33 patients with HER2-positive metastatic breast cancer (MBC) and available tumor samples treated with a trastuzumab-based regimen, we retrospectively performed dual-color fluorescence in-situ hybridization test ...

journal_title：Investigational new drugs

authors： Gullo G,Bettio D,Torri V,Masci G,Salvini P,Santoro A

更新日期：2009-04-01 00:00:00

abstract：:We studied the effect of riccardin D, a macrocyclic bisbibenzyl, which was isolated from the Chinese liverwort plant, on human leukemia cells and the underlying molecular mechanism. Riccardin D had a significant antiproliferative effect on human leukemia cell lines HL-60, K562 and its multidrug resistant (MDR) counter...

journal_title：Investigational new drugs

authors： Xue X,Qu XJ,Gao ZH,Sun CC,Liu HP,Zhao CR,Cheng YN,Lou HX

更新日期：2012-02-01 00:00:00

abstract：:Cis-diaminechloro-[2-(diethylamino) ethyl 4-amino-benzoate, N(4)]-chloride platinum (II) monohydrochloride monohydrate (DPR) is a new platinum triamine complex obtained from the synthesis of cisplatin and procaine. In this paper we analyzed, adopting a disease-oriented strategy, the tumour selectivity of this compound...

journal_title：Investigational new drugs

authors： Mariggiò MA,Cafaggi S,Ottone M,Parodi B,Vannozzi MO,Mandys V,Viale M

更新日期：2004-01-01 00:00:00

abstract：:4-demethoxydaunorubicin (4-dm DNR), a new analog of daunorubicin, was tested at an every 3-week dose schedule in 63 evaluable patients with various forms of disseminated malignancy. Utilizing the intravenous (i.v.) route of administration, the maximum tolerated dose (MTD) was 15-18 mg/m2; with the oral route the MTD w...

journal_title：Investigational new drugs

authors： Bonfante V,Ferrari L,Villani F,Bonadonna G

更新日期：1983-01-01 00:00:00

abstract：:Antiprogestins have been largely utilized in reproductive medicine, yet their repositioning for oncologic use is rapidly emerging. In this study we investigated the molecular mediators of the anti-ovarian cancer activity of the structurally related antiprogestins RU-38486, ORG-31710 and CDB-2914. We studied the respon...

journal_title：Investigational new drugs

authors： Goyeneche AA,Seidel EE,Telleria CM

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND:To explore the activity of lapatinib with a novel trial design focused on the drug target rather than on histology. METHODS:Patients with HER2 amplified gastro-esophageal, bladder, ovarian, or uterine tumors were enrolled into a double-blinded randomized discontinuation study of lapatinib 1,500 mg PO daily....

journal_title：Investigational new drugs

authors： Galsky MD,Von Hoff DD,Neubauer M,Anderson T,Fleming M,Nagarwala Y,Mahoney JM,Midwinter D,Vocila L,Zaks TZ

更新日期：2012-04-01 00:00:00

abstract：:Neuroblastoma is an extracranial, solid, and heterogeneous malignancy in children. The conventional therapeutic modalities are mostly ineffective and thus new therapeutic strategies for malignant neuroblastoma are urgently warranted. We examined the synergistic efficacy of combination of sorafenib (SF) and genistein (...

journal_title：Investigational new drugs

authors： Roy Choudhury S,Karmakar S,Banik NL,Ray SK

更新日期：2010-12-01 00:00:00

abstract：:Purpose Preclinical evidence suggests dichloroacetate (DCA) can reverse the Warburg effect and inhibit growth in cancer models. This phase 1 study was undertaken to assess the safety, recommended phase 2 dose (RP2D), and pharmacokinetic (PK) profile of oral DCA in patients with advanced solid tumors. Patients and Meth...

journal_title：Investigational new drugs

authors： Chu QS,Sangha R,Spratlin J,Vos LJ,Mackey JR,McEwan AJ,Venner P,Michelakis ED

更新日期：2015-06-01 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：:Anthracycline antibiotics (ANT), such as doxorubicin or daunorubicin, are a class of anticancer drugs that are widely used in oncology. Although highly effective in cancer therapy, their usefulness is greatly limited by their cardiotoxicity. Possible mechanisms of ANT cardiotoxicity include their conversion to seconda...

journal_title：Investigational new drugs

authors： Piska K,Koczurkiewicz P,Bucki A,Wójcik-Pszczoła K,Kołaczkowski M,Pękala E

更新日期：2017-06-01 00:00:00

abstract：:The matrix metalloproteinases (MMPs) are a family of at least fifteen secreted and membrane-bound zinc-endopeptidases. Collectively, these enzymes can degrade all of the components of the extracellular matrix, including fibrallar and non-fibrallar collagens, fibronectin, laminin and basement membrane glycoproteins. MM...

journal_title：Investigational new drugs

authors： Wojtowicz-Praga SM,Dickson RB,Hawkins MJ

更新日期：1997-01-01 00:00:00

abstract：:LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest. Screening in the NCI60 cancer cell lines resulted in a mean GI50 of approximately 100 nM. Here, we report the results of testing in multiple mouse xenograft models and angiogenesis assays, along wit...

journal_title：Investigational new drugs

authors： Gardner ER,Kelly M,Springman E,Lee KJ,Li H,Moore W,Figg WD

更新日期：2012-02-01 00:00:00

abstract：OBJECTIVE:Everolimus (RAD001) is a novel mammalian target of rapamycin (mTOR) inhibitor, and anti-proliferative activity in various malignancies has been reported. This study evaluated the anti-tumor effects and schedule-dependent synergism of everolimus in combination with other chemotherapeutic agents in T-cell lymph...

journal_title：Investigational new drugs

authors： Huang JJ,Li ZM,Huang Y,Huang Y,Tian Y,He XX,Xiao J,Lin TY

更新日期：2012-02-01 00:00:00

abstract：:A phase II trial of 4' Deoxydoxorubicin (DXDX) was conducted in unresectable previously untreated non-small cell lung cancer patients. DXDX was administered every 3 weeks by short intravenous infusion at a starting dose of 30 mg/m2, with dose escalation to 40 mg/m2 toxicity permitting. Four responses, all partial, wer...

journal_title：Investigational new drugs

authors： Rose C,Lad TE,Kilton LJ,Schor J,Rosen ST,Rossof AH,Blough RR,Johnson CM

更新日期：1990-02-01 00:00:00

abstract：:Tyrosine kinase inhibitors (TKI) or monoclonal antibodies targeting EGFR, HER2 or VEGFR receptors have demonstrated substantial clinical benefit in patients with advanced breast cancer, colon cancer, head and neck cancer, non-small cell lung cancer, and renal cell carcinoma. Nevertheless, these drugs have some target ...

journal_title：Investigational new drugs

authors： Bahleda R,Massard C,Soria JC,Izzedine H,Cohen A,Ederhy S

更新日期：2010-06-01 00:00:00

abstract：:In an on-going Phase II evaluation, dianhydrogalactitol (NSC 132313) was administered intravenously to 28 patients with advanced or recurrent non-squamous cell carcinoma of the cervix. The initial dosage was 60 mg/m2/wk with escalation to 75 mg/m2/wk if there were no adverse effects. Twenty-seven patients were evaluab...

journal_title：Investigational new drugs

authors： Stehman FB,Blessing JA,Homesley HD,Currie JL,Yordan EL

更新日期：1984-01-01 00:00:00

abstract：:This study was conducted to assess the efficacy and toxicity of suramin administered using a fixed dose schedule in patients with advanced renal cell carcinoma. Fourteen eligible patients with advanced renal cell carcinoma were enrolled and treated on a fixed dose schedule of suramin administered over 12 weeks. Surami...

journal_title：Investigational new drugs

authors： Dreicer R,Smith DC,Williams RD,See WA

更新日期：1999-01-01 00:00:00

abstract：:Rolapitant is a neurokinin-1 receptor antagonist that is approved in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting (CINV) associated with initial and repeat courses of emetogenic cancer chemotherapy, including but not limited to highly emetogenic chemotherapy. Her...

journal_title：Investigational new drugs

authors： Zhang ZY,Wang J,Kansra V,Wang X

更新日期：2019-02-01 00:00:00

abstract：:9-Aminocamptothecin (9-AC) is a water-insoluble camptothecin derivative that demonstrated broad activity in pre-clinical studies. In vitro, greater anti-tumor efficacy can be achieved with prolonged administration. A minor response was observed in gastric cancer in a phase I study. We conducted a phase II study of 9-A...

journal_title：Investigational new drugs

authors： Kindler HL,Avadhani A,Wade-Oliver K,Karrison T,Mani S,Vokes EE

更新日期：2004-08-01 00:00:00

abstract：:Flavone acetic acid (FAA) was incubated for 1 to 48 hr with 3 established human colon cancer cell lines endowed with distinct degrees of phenotypic properties. All 3 lines responded to FAA in almost identical fashion; when incubated with the drug for only 1 hr, an initial decrease in survival was observed for concentr...

journal_title：Investigational new drugs

authors： Drewinko B,Yang LY

更新日期：1986-01-01 00:00:00

abstract：:Sixteen patients with stage IV melanoma, who were heavily pretreated, received 11 mg/m2/day of intravenous Irofulven for five consecutive days every 28 days. There were no objective tumor responses, although one patient exhibited stable disease after 4 cycles. The most common toxicities were grade 1/2 nausea, vomiting...

journal_title：Investigational new drugs

authors： Pierson AS,Gibbs P,Richards J,Russ P,Eckhardt SG,Gonzalez R

更新日期：2002-08-01 00:00:00

abstract：BACKGROUND:This study investigated the activity of MK-2206, an AKT inhibitor, in metastatic or recurrent nasopharyngeal carcinoma (NPC). METHOD:Oral MK-2206 at a dose of 200 mg was administered on days 1, 8, 15 and 22 of a 28-day cycle until progression. Plasma EBV DNA clearance during the first month of treatment was...

journal_title：Investigational new drugs

authors： Ma BB,Goh BC,Lim WT,Hui EP,Tan EH,Lopes Gde L,Lo KW,Li L,Loong H,Foster NR,Erlichman C,King AD,Kam MK,Leung SF,Chan KC,Chan AT

更新日期：2015-08-01 00:00:00