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Restrict the search for
telotristat ethyl
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
IZONSTERIDE, a benzoquinolinone, is a selective inhibitor of the 5-alpha reductase, with antagonistic effect on both the type I (liver, skin, hair follicles) and type II (prostate) isoforms of the enzyme. It is a competitive inhibitor of type I 5-alpha reductase and a non-competitive inhibitor of type II 5-alpha reductase. It was under development for the treatment of prostatic cancer.
Status:
Investigational
Source:
NCT00082368: Phase 2 Interventional Completed Cancer
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tariquidar, a non-competitive, specific P-glycoprotein (Pgp) inhibitor, is an anthranilamide derivative with multidrug resistance properties. Tariquidar binds to the ATP-binding cassette (ABC) transport protein Pgp, thereby inhibiting transmembrane transport of anticancer drugs resulting in their increased intracellular concentrations augmenting cytotoxicity of an anticancer drug. Tariquidar was discovered by Xenova Group and was developed for the treatment of multidrug resistance in cancer. In October 2002 the US Food
and Drug Administration (FDA) has granted fast track review status to tariquidar for the treatment of multi-drug resistance in first-line treatment of non-small cell lung cancer (NSCLC) patients. Tariquidar is still undergoing research as an adjuvant against multidrug resistance in cancer.
Class (Stereo):
CHEMICAL (ACHIRAL)
FLUALAMIDE is an antiemetic agent.
Status:
Investigational
Source:
NCT00319748: Phase 2 Interventional Completed Breast Cancer
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
CPG-52852 (PF-04878691) is a toll-like receptor 7 (TRL7) agonist. The drug was developed by 3M Pharmaceuticals and the Coley Pharmaceutical Group and was investigated in a number of clinical trials in patients with advanced cancer. Sustained tolerability and modest clinical benefit were demonstrated in heavily pretreated recurrent breast, ovarian, and cervix cancers. After Coley was acquired by Pfizer in 2007, the drug was repurposed for the treatment of hepatitis C. A phase 1 clinical trial was conducted. The development of the compound was discontinued because the compound was believed to unlikely to achieve the proof-of-concept criteria as a result of pharmacodynamic modeling.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Murabutide is a safe synthetic immunomodulator derived from muramyl dipeptide, the smallest bioactive unit of bacterial peptidoglycan. In contrast to muramyl dipeptide, Murabutide is devoid of pyrogenic activity and lacks somnogenic activity. Murabutide acts as a ligand for the intracellular receptor NOD2 and has the capacity to synergize with selected therapeutic cytokines to drive the release of Th1 cytokines. Murabutide has been found to suppress human immunodeficiency virus type-1 (HIV-1) replication, in macrophages, through regulated expression of cellular factors needed at different steps in the virus replication cycle.
Class (Stereo):
CHEMICAL (ACHIRAL)
Elbanizine [HWA 214] is an antihistamine which was undergoing preclinical trials with Hoechst Marion Roussel in Germany for the treatment of allergic asthma. Elbanizine does not have such drawbacks as causing drowsiness or being effective only as a prophylactic drug, and could provide advantages over other non-sedative compounds, such as terfenadine and astemizole, in that it is water soluble and thus can be administered through inhalation or through intravenous application.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Etomoxir is an irreversible inhibitor of carnitine O-palmitoyltransferase (CPT) I. It inhibits fatty acid oxidation and fatty acid and cholesterol synthesis in an enantiomer-selective manner: only the R-enantiomer of etomoxir inhibits fatty acid oxidation, S-enantiomer inhibits fatty acid and cholesterol synthesis but not fatty acid oxidation. Etomoxir was studied for the treatment of congestive heart failure and type II diabetes, however, its development was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Pinafide is a rodenticide and anti-protozoal agent. Pinafide shows strong cytostatic activity against both HeLa and KB cells and is moderately toxic to both mice and rats. It has been proved active against experimental tumors and shown to be inhibitor of two DNA viruses. Pinafide blocks cell growth by inhibiting DNA and RNA synthesis. It has been shown to bind to double-helical DNA by intercalation. Pinafide inhibited the activity of M. tuberculosis NAD⁺-dependent DNA ligase A at concentrations of 50 uM. At the chemical screening was found that pinafide inhibited B-Myb transcriptional activity in luciferase assays. The cross placental-barrier studies showed that 3H-pinafide was present in the 14-day fetuses.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ersentilide (CK-3579 or HE93) is a blocker of beta1-adrenergic receptors and potassium channels. It exerts class III antiarrhythmic activity. It prevents ventricular fibrillation in a canine model of lethal arrhythmias.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Erbulozole (R 55104) is a water soluble congener of the microtubule inhibitor tubulozole, which has proven to possess anti-invasive, antitumoral and radiosensitizing capacities. Erbulozole development for the treatment of cancer has been discontinued.
