U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 4211 - 4220 of 4747 results

Status:
Investigational
Source:
NCT01168791: Phase 3 Interventional Completed Soft Tissue Sarcoma
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Palifosfamide or ZIO-201 (isophosphoramide mustard; IPM), a bi-functional DNA alkylator, is the active metabolite of ifosfamide (IFOS). IFOS and the related drug cyclophosphamide (CPA) are widely used anti-cancer drugs. Both are pro-drugs and need to be metabolized to be active. Their clinical use is limited by the toxicity associated with some of their metabolites. Palifosfamide has shown efficacy in diverse cancer models. ZIOPHARM Oncology Inc, under license from Dekk-Tec Inc, was developing palifosfamide, a formulation of isophosphoramide mustard with tris(hydroxymethyl)aminomethane salt-stabilization (palifosfamide-tris) and previously with lysine-stabilization (palifosfamide-lys). Preclinical studies and phase I and I/II clinical trials demonstrated that palifosfamide-tris had an antitumor efficiency comparable or superior to that of ifosfamide. To date ZIO-201 is not present in ZIOPHARM pipeline.
Status:
Investigational
Source:
NCT02860000: Phase 2 Interventional Active, not recruiting Estrogen Receptor Status
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. Alisertib inhibited AAK over ABK with a selectivity of more than 200-fold in cells and produced a dose-dependent decrease in bipolar and aligned chromosomes in the HCT-116 xenograft model, a phenotype consistent with AAK inhibition. Alisertib inhibited proliferation of human tumor cell lines in vitro and produced tumor growth inhibition in solid tumor xenograft models and regressions in in vivo lymphoma models. It is currently in phase II clinical trials for acute myeloid leukaemia; B cell lymphoma; brain cancer; mesothelioma; prostate cancer; small cell lung cancer.
Status:
Investigational
Source:
NCT00273884: Phase 2 Interventional Completed Acute Myeloid Leukemia
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Amonafide L-malate (AS1413, Xanafide) is a DNA intercalator and topoisomerase II inhibitor that induces apoptosis by disrupting chromatin organisation independently of ATP. This is different from classical topoisomerase II inhibitors which induce apoptosis by causing extensive DNA damage. Amonafide L-malate is also able to evade P-glycoprotein and related transporters that contribute to multi-drug resistance. AS1413 had orphan drug status in both the U.S. and the E.U. for the treatment of AML and also received Fast Track status from the U.S. FDA for the treatment of secondary AML. Amonafide L-malate was originated by Xanthus Pharmaceuticals. It was added to Antisoma's pipeline through the acquisition of Xanthus Pharmaceuticals, Inc. in June 2008. Antisoma discontinued development of Amonafide L-malate after data from the open-label, international Phase III ACCEDE trial in over 420 patients showed that 600 mg/m 2 IV amonafide for 5 days plus cytarabine missed the primary endpoint of significantly improving initial remission rate, defined as the proportion of patients who achieve CR or CRi, vs. daunorubicin plus cytarabine.
P276-00 (also known as riviciclib) is a novel, potent, small-molecule, flavone-derived inhibitor of cyclin-dependent kinases (Cdk), Cdk 4 D1, Cdk1 B, and Cdk9 T, with potent cytotoxic effects against chemosensitive and chemoresistant cancer cell lines. P276-00 was in phase II clinical trial for the treatment mantle cell lymphoma, but that study was terminated based on interim results and all subjects were off study at that time. Although, there were not the major safety or tolerability concerns. However, this drug successfully passed phase II clinical trial for the treatment Melanoma, squamous cell carcinoma of head and neck, malignant melanoma and in combination with Gemcitabine in the treatment of advanced pancreatic cancer.
Status:
Investigational
Source:
INN:acetorphine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Acetorphine is a synthetic narcotic analgesic. Acetorphine was reported to have uses in veterinary medicine with pronounced advantages in the immobilization of the giraffe in which toxic effects were reduced as compared to the effects of etorphine. In July 1966, the Director-General of the World Health Organization informed the Secretary-General that WHO had arrived at the conclusion that etorphine and acetorphine should be included in Schedule I of the Convention, since they could give rise to similar abuse, and produce similar ill effects as the substances already listed therein. Acetorphine is a Schedule I controlled substance in the United States.
Status:
Investigational
Source:
NCT02860000: Phase 2 Interventional Active, not recruiting Estrogen Receptor Status
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. Alisertib inhibited AAK over ABK with a selectivity of more than 200-fold in cells and produced a dose-dependent decrease in bipolar and aligned chromosomes in the HCT-116 xenograft model, a phenotype consistent with AAK inhibition. Alisertib inhibited proliferation of human tumor cell lines in vitro and produced tumor growth inhibition in solid tumor xenograft models and regressions in in vivo lymphoma models. It is currently in phase II clinical trials for acute myeloid leukaemia; B cell lymphoma; brain cancer; mesothelioma; prostate cancer; small cell lung cancer.
Status:
Investigational
Source:
INN:cethexonium chloride
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Cethexonium is a cyclohexanols derivative with antimicrobial activities.
Status:
Investigational
Source:
NCT02260648: Phase 3 Interventional Terminated Hypercholesterolemia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Evacetrapib (LY2484595) is a novel benzazepine-based CETP inhibitor that has been developed at Lilly Research Laboratories. Evacetrapib inhibits CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3. On 01 Sep 2016 Eli Lilly terminates the phase III ACCENTUATE trial in Hyperlipidaemia (Adjunctive treatment) in USA and Puerto Rico (PO) due to insufficient efficacy (NCT02227784).
Status:
Investigational
Source:
NCT04090736: Phase 3 Interventional Active, not recruiting Leukemia, Myeloid, Acute
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pevonedistat (MLN4924), discovered by Millennium, is a small molecule inhibitor of the NEDD8-Activating Enzyme (NAE), a key component of the protein homeostasis pathway. MLN4924 is a mechanism-based inhibitor of NAE and creates a covalent NEDD8-MLN4924 adduct catalyzed by the enzyme. The NEDD8-MLN4924 adduct resembles NEDD8 adenylate, the first intermediate in the NAE reaction cycle, but cannot be further utilized in subsequent intraenzyme reactions. The stability of the NEDD8-MLN4924 adduct within the NAE active site blocks enzyme activity, thereby accounting for the potent inhibition of the NEDD8 pathway by MLN4924. This drug is in phase II clinical trial for the treatment acute myeloid leukemia, chronic myelomonocytic leukemia and myelodysplastic syndromes. In addition in phase I for treatment acute lymphoblastic leukemia. The ability of MLN4924 to cross the blood-brain barrier, its low toxicity, and clinical efficacy in other cancers suggests that this drug is an attractive treatment against glioblastomas.
Status:
Investigational
Source:
NCT00805805: Phase 3 Interventional Completed Primary Biliary Cirrhosis
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Showing 4211 - 4220 of 4747 results