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Status:
Investigational
Source:
NCT01002963: Phase 1 Interventional Completed Healthy
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist. It is used as a tool compound to study involvement of EP2 receptor in various pathologies. In combination with EP4 antagonist, PF-04418948 attenuates PGE2-induced airway microvascular leak in model of asthma, and PGE2-induced gut dismotility.
Status:
Investigational
Source:
NCT02311933: Phase 2 Interventional Active, not recruiting Recurrent Breast Carcinoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is active metabolites of tamoxifen. This metabolite exhibits a 100-fold higher binding affinity to the estrogen receptor (ER) and are more effective in suppressing cell proliferation than tamoxifen. In humans, the conversion from tamoxifen to endoxifen is predominant. Endoxifenis is an orally active, selective estrogen receptor modulator (SERM) that was developed for the treatment of estrogen receptor-positive breast cancer. In addition, this drug possesses antimanic properties, what can be used in the treatment of patients with bipolar I disorder (BPD I).
Status:
Investigational
Source:
NCT02377336: Phase 2 Interventional Withdrawn Ischemic Heart Disease
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Eleclazine (formerly known as GS-6615) is a dihydrobenzoxazepinone selective cardiac late sodium current inhibitor. Gilead Sciences is developing eleclazine as an oral treatment for long QT syndrome, hypertrophic cardiomyopathy, ischaemic heart disease, and Ventricular arrhythmias.
Status:
Investigational
Source:
NCT01807026: Phase 1 Interventional Completed Alzheimer Disease
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
LY2886721 is a BACE inhibitor used for the treatment of Alzheimer's Disease. LY2886721 did not inhibit other aspartyl proteases such as cathepsin D, pepsin, and renin, and reduced Aβ in a dose-dependent manner in HEK293Swe cells and in primary neurons from PDAPP transgenic mice. LY2886721 was the first BACE inhibitor to reach Phase 2 clinical research. Lilly completed six Phase 1 studies of LY2886721’s safety, tolerability, and pharmacology in a total of 150 healthy volunteers and people with Alzheimer’s disease at doses of 1–70 mg. Single and multiple ascending oral dosing was accompanied by repeat CSF sampling in the hours and days thereafter. This was done to assess CSF penetration and target engagement by way of measuring levels of the drug, BACE1 substrate, and BACE1 cleavage products. The compound lowered CSF Aβ40, Aβ42, and sAPPβ concentrations while increasing sAPPα, consistent with expectations for BACE1 inhibition. Fourteen days of daily dosing reduced BACE1 activity by 50–75 percent, and CSF Aβ42 by 72 percent. No safety concerns were apparent in dosing up to six weeks
Status:
Investigational
Source:
NCT00046696: Phase 1 Interventional Completed Neoplasms
(2001)
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
1H-2-BENZOPYRAN-3-ACETIC ACID, 8-HYDROXY-6-METHOXY-Α-METHYL-1-OXO- (NM-3) is an orally bioavailable antiangiogenic isocoumarin with potential antineoplastic activity. NM-3 inhibits vascular endothelial growth factor (VEGF), a pro-angiogenic growth factor, thereby inhibiting endothelial cell proliferation. NM-3 induces apoptosis by a mechanism involving reactive oxygen species. In human MCF-7 and ZR-75-1 breast cancer cells, NM-3 induces the p21 cyclin-dependent kinase inhibitor, cell cycle arrest at G1-S-phase, and necrotic cell death. NM-3 has been used in trials studying the treatment of solid tumours.
Status:
Investigational
Source:
NCT02467023: Not Applicable Interventional Completed Sepsis
(2015)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Status:
Investigational
Source:
NCT00838461: Phase 1 Interventional Completed Healthy Subjects
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
HSD-016 was discovered as an orally efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of diabetes. The phase I in clinical trials for the drug was completed; however, information about further studies is not available.
Status:
Investigational
Source:
NCT02013310: Phase 2 Interventional Completed Age-Associated Memory Impairment (AAMI)
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Inflazyme Pharmaceuticals initially developed HT-0712 as a phosphodiesterase IV (PDE4) inhibitor with anti-inflammatory properties. Now the rights on this drug are wholly owned by Dart NeuroScience. January 2015, Dart NeuroScience completed a phase II trial of HT-0712 for the memory disorders, where were evaluated the efficacy in improving memory and cognitive performance.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Etocrylene is an organic ester that appears as an off-white crystalline powder and functions as a UV absorber. When applied to the skin, this product absorbs UV rays. It can also be used to protect cosmetics and personal care products from deterioration. This product can be used in the formulation of sun protection products, as well as bath, skin, cleansing, hair, nail and fragrance products.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Trequinsin is a potent PDE3 inhibitor that inhibits PDE4 and PDE2 at higher concentrations. Trequinsin can block platelet aggregation and also inhibit tissue factor expression in human endothelial cells. Trequinsin can enhance cellular cAMP content, forskolin-induced cAMP synthesis, and renin release in cells.