Nafazatrom: clonogenic in-vitro assessment of activity against human malignancies.

abstract：:Sorafenib, an orally active multi-kinase inhibitor approved for the treatment of hepatocellular carcinoma (HCC), is primarily metabolized both via cytochrome P450 3A4 isoform (CYP3A4) and UGT1A9. Due to the contribution of these two biotransformation pathways, sorafenib is considered to be less susceptible than other ...

journal_title：Investigational new drugs

authors： Gomo C,Coriat R,Faivre L,Mir O,Ropert S,Billemont B,Dauphin A,Tod M,Goldwasser F,Blanchet B

更新日期：2011-12-01 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：:Radioactive iodine-refractory [(18)F] fluorodeoxy-glucose-positron emission tomography-positive thyroid carcinomas represent especially aggressive tumors. Targeting glucose metabolism by the transketolase isoenzyme transketolase like 1 (TKTL-1) which is over-expressed in various neoplasms, may be effective. The correl...

journal_title：Investigational new drugs

authors： Fröhlich E,Fink I,Wahl R

更新日期：2009-08-01 00:00:00

abstract：:Background Treatment of recurrent, unresectable granulosa cell tumor (GCT) of the ovary can be challenging. Given the rarity of the tumor, alternative therapies have been difficult to evaluate in large prospective clinical trials. Currently, to our knowledge, there are no reports of the use of immune checkpoint inhibi...

journal_title：Investigational new drugs

authors： How JA,Jazaeri A,Westin SN,Sood AK,Ramondetta LM,Xu M,Abonofal A,Karp DD,Subbiah V,Stephen B,Rodon JA,Yang F,Naing A

更新日期：2021-01-07 00:00:00

abstract：:Ninety per cent of pancreatic adenocarcinomas (PC) contain mutations of the K-Ras proto-oncogene resulting in constitutively activated Ras protein. A critical step in Ras activation is farnesylation of Ras protein. Farnesyl transferase inhibitors are compounds that inhibit farnesylation. We report the results of a pha...

journal_title：Investigational new drugs

authors： Macdonald JS,McCoy S,Whitehead RP,Iqbal S,Wade JL 3rd,Giguere JK,Abbruzzese JL

更新日期：2005-10-01 00:00:00

abstract：:Interleukin-4 (IL-4) is a pleiotropic cytokine affecting growth and differentiation of various cell types as well as regulating other cytokines. To study the effect of IL-4 on AIDS-related Kaposi's sarcoma (AIDS-KS) cells, we first examined the tumor cells for IL-4 receptor (IL-4R) expression. KS cells express a singl...

journal_title：Investigational new drugs

authors： Cai J,Zheng T,Murphy J,Waters CA,Lin GY,Gill PS

更新日期：1997-01-01 00:00:00

abstract：PURPOSE:Preclinical data indicate that combination HER2-directed and anti-VEGF therapy may bypass resistance to trastuzumab. A phase I trial was performed to assess safety, activity, and correlates. EXPERIMENTAL DESIGN:Patients with advanced, refractory malignancy were enrolled (modified 3 + 3 design with expansions f...

journal_title：Investigational new drugs

authors： Falchook GS,Moulder S,Naing A,Wheler JJ,Hong DS,Piha-Paul SA,Tsimberidou AM,Fu S,Zinner R,Janku F,Jiang Y,Huang M,Parkhurst KL,Kurzrock R

更新日期：2015-02-01 00:00:00

abstract：:Background PF-06650808 is a novel anti-Notch3 antibody-drug conjugate (ADC) able to deliver an auristatin-based cytotoxic payload to target cells. In this first-in-human, dose-finding, phase I study (NCT02129205), we investigated safety, pharmacokinetics, immunogenicity, and preliminary antitumor activity of single-ag...

journal_title：Investigational new drugs

authors： Rosen LS,Wesolowski R,Baffa R,Liao KH,Hua SY,Gibson BL,Pirie-Shepherd S,Tolcher AW

更新日期：2020-02-01 00:00:00

abstract：PURPOSE:This study investigated the maximum-tolerated dose (MTD), dose-limiting toxicity (DLT), and pharmacokinetic (PK) profiles of DHP107, a novel oral paclitaxel containing neither Cremophor EL nor P-glycoprotein (P-gp) inhibitor. PATIENTS AND METHODS:Patients with advanced solid tumors refractory to all standard t...

journal_title：Investigational new drugs

authors： Hong YS,Kim KP,Lim HS,Bae KS,Ryu MH,Lee JL,Chang HM,Kang YK,Kim H,Kim TW

更新日期：2013-06-01 00:00:00

abstract：:The anti-tumor properties of novel derivatives prepared from Aconitum C(20)-diterpenoid alkaloid, which show the least toxicity among the Aconitum alkaloids, were investigated in the Non-Hodgkin's lymphoma cell line Raji cells. Two novel Aconitum C(20)-diterpenoid alkaloid derivatives, 11-m-Trifluorometylbenzoyl (Mb)-...

journal_title：Investigational new drugs

authors： Hazawa M,Takahashi K,Wada K,Mori T,Kawahara N,Kashiwakura I

更新日期：2011-02-01 00:00:00

abstract：:This study was designed to test the hypothesis that specific inhibition of cathepsins B and L will cause death of neuroblastoma cells. Five compounds that differ in mode and rate of inhibition of these two enzymes were all shown to cause neuroblastoma cell death. Efficacy of the different compounds was related to thei...

journal_title：Investigational new drugs

authors： Cartledge DM,Colella R,Glazewski L,Lu G,Mason RW

更新日期：2013-02-01 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：:Mitonafide is the lead compound of a new series of antitumor drugs, the 3-Nitronaphthalimides, which have shown antineoplastic activity in vitro as well as in vivo. This phase I Mitonafide study in non-small cell lung cancer using a 120-hour continuous infusion (120 h. C.I.) schedule of administration was designed to ...

journal_title：Investigational new drugs

authors： Rosell R,Carles J,Abad A,Ribelles N,Barnadas A,Benavides A,Martin M

更新日期：1992-08-01 00:00:00

abstract：:Background To determine the recommended dose (RD) of a combination of PM01183 and gemcitabine in patients with advanced solid tumors. Methods Forty-five patients received escalating doses of PM01183/gemcitabine on Days 1 and 8 every 3 weeks (d1,8 q3wk) following a standard 3 + 3 design. Results PM01183 3.5 mg flat dos...

journal_title：Investigational new drugs

authors： Paz-Ares L,Forster M,Boni V,Szyldergemajn S,Corral J,Turnbull S,Cubillo A,Teruel CF,Calderero IL,Siguero M,Bohan P,Calvo E

更新日期：2017-04-01 00:00:00

abstract：INTRODUCTION:Heat shock protein 90 (Hsp90) has been studied as a therapeutic target in many cancers. In preclinical trials, the Hsp90 ATPase inhibitor ganetespib demonstrated potent inhibition of solid tumor growth, with superior potency than prior Hsp90 inhibitors. Given the promising preclinical outcome and favorable...

journal_title：Investigational new drugs

authors： Thakur MK,Heilbrun LK,Sheng S,Stein M,Liu G,Antonarakis ES,Vaishampayan U,Dzinic SH,Li X,Freeman S,Smith D,Heath EI

更新日期：2016-02-01 00:00:00

abstract：:We investigated proliferation and apoptosis induction in Jurkat T-leukemia cells by the new isothiocyanate 4-(methylthio)butylisothiocyanate (MTBITC). To help elucidate whether the effects of MTBITC are specific for cancer cells, we tested MTBITC on freshly isolated, non-transformed human peripheral T lymphocytes. The...

journal_title：Investigational new drugs

authors： Fimognari C,Nüsse M,Iori R,Cantelli-Forti G,Hrelia P

更新日期：2004-04-01 00:00:00

abstract：:Twenty-four evaluable patients with epithelial ovarian cancer resistant to primary therapy, or relapsing after response to initial therapy, were treated with acivicin utilizing a daily X 5 schedule. One patient achieved a partial response lasting five months; the remaining 23 patients showed no objective response. Pro...

journal_title：Investigational new drugs

authors： McGuire WP,Blessing JA,DiSaia PJ,Buchsbaum HJ

更新日期：1986-01-01 00:00:00

abstract：:Fifteen patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck received a 5 day continuous I.V. infusion of 6-thioguanine repeated every five weeks. Dose limiting toxicity was primarily hematological with grade III/IV leucopenia and thrombocytopenia seen in seven patients. Nausea and vo...

journal_title：Investigational new drugs

authors： Kruter F,Eisenberger M,Sinibaldi V,Engstrom C,Jacobs M,Abrams J,Belani C,Gray W,Krasnow S

更新日期：1992-07-01 00:00:00

abstract：:Standard therapy for advanced or metastatic non-small cell lung cancer (NSCLC) has primarily consisted of traditional cytotoxic chemotherapy, although use of targeted therapies has been approved in specific settings. Antiangiogenic agents represent a promising therapeutic strategy for treatment of advanced NSCLC. Beva...

journal_title：Investigational new drugs

authors： Blumenschein GR Jr

更新日期：2012-08-01 00:00:00

abstract：:Bombesin/gastrin-releasing peptides (BN/GRP) were shown to bind selectively to cell surface receptors, stimulating the growth of various types of malignancies in murine and human models. The novel BN/GRP synthetic receptor antagonist, RC-3095, was able to produce long-lasting tumor regressions in murine and human tumo...

journal_title：Investigational new drugs

authors： Schwartsmann G,DiLeone LP,Horowitz M,Schunemann D,Cancella A,Pereira AS,Richter M,Souza F,da Rocha AB,Souza FH,Pohlmann P,De Nucci G

更新日期：2006-09-01 00:00:00

abstract：:Preclinical studies, along with Phase I, II, and III clinical trials demonstrate the pharmacokinetics, pharmacodynamics, safety and efficacy of a new drug under well controlled circumstances in relatively homogeneous populations. However, these types of studies generally do not answer important questions about variabi...

journal_title：Investigational new drugs

authors： Blesch KS,Gieschke R,Tsukamoto Y,Reigner BG,Burger HU,Steimer JL

更新日期：2003-05-01 00:00:00

abstract：OBJECTIVE:To determine the recommended dose for phase II trials of elisidepsin (PM02734, Irvalec®) in combination with erlotinib in patients with advanced malignant solid tumors. METHODS:Open-label, dose-escalating, phase I study of intravenous elisidepsin administered weekly (days 1, 8 and 15) over 3 h as a flat dose...

journal_title：Investigational new drugs

authors： Goel S,Viteri S,Morán T,Coronado C,Dios JL,Miguel-Lillo B,Fernández-García EM,Rosell R

更新日期：2016-02-01 00:00:00

abstract：:Virotherapy is an emerging strategy for the treatment of cancer that utilizes both replication-competent and genetically modified viruses to selectively kill tumor cells. We have previously shown that Coxsackievirus A21 (CVA21), a common-cold producing enterovirus, is an effective oncolytic agent against human melanom...

journal_title：Investigational new drugs

authors： Skelding KA,Barry RD,Shafren DR

更新日期：2012-04-01 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：:Ninhydrin (2,2-dihydroxy-1,3-indane dione) was evaluated for its antitumor and cytotoxic properties in Ehrlich ascites carcinoma cell (EAC Cell)-bearing mice. The rationale behind this study has been mainly the literature reports of its characteristic interference with DNA synthesis and calcium homeostasis. Antitumor ...

journal_title：Investigational new drugs

authors： Qureshi S,Al-Shabanah OA,Al-Bekairi AM,Al-Harbi MM,Al-Gharably NM,Raza M

更新日期：2000-08-01 00:00:00

abstract：BACKGROUND:Foretinib is a small-molecule, oral multikinase inhibitor primarily targeting the mesenchymal epithelial transition (MET) factor receptor, and the vascular endothelial growth factor receptor 2. We conducted a phase II study to evaluate the single-agent activity and tolerability of foretinib in patients with ...

journal_title：Investigational new drugs

authors： Seiwert T,Sarantopoulos J,Kallender H,McCallum S,Keer HN,Blumenschein G Jr

更新日期：2013-04-01 00:00:00

abstract：:The (6-maleimidocaproyl)hydrazone derivative of doxorubicin (INNO-206) is an albumin-binding prodrug of doxorubicin with acid-sensitive properties that is being assessed clinically. The prodrug binds rapidly to circulating serum albumin and releases doxorubicin selectively at the tumor site. This novel mechanism may p...

journal_title：Investigational new drugs

authors： Graeser R,Esser N,Unger H,Fichtner I,Zhu A,Unger C,Kratz F

更新日期：2010-02-01 00:00:00

abstract：:Trimetrexate (TMTX) is an analog of methotrexate and a potent inhibitor of the enzyme dihydrofolate reductase. In this phase I study, TMTX was given intravenously to 32 patients as a constant infusion over 24 hours every 28 days. The maximum-tolerated dose of TMTX was 200 mg/m2, with myelosuppression as the dose-limit...

journal_title：Investigational new drugs

authors： Allegra CJ,Jenkins J,Weiss RB,Balis F,Drake JC,Brooks J,Thomas R,Curt GA

更新日期：1990-05-01 00:00:00

abstract：:Mezerein, the most active antitumor compound isolated from the daphne species of plants, has a structural similarity to phorbol myristate acetate (PMA), the major active compound isolated from croton oil. PMA is known to have tumor promoting activity and is a potent inflammatory agent. Mezerein has similarly been repo...

journal_title：Investigational new drugs

authors： Barton K,Randall G,Sagone AL Jr

更新日期：1989-07-01 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