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Restrict the search for
vitamin a
to a specific field?
Status:
Investigational
Source:
NCT01184508: Phase 2 Interventional Terminated Migraine Headache
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
LY2300559 is a dual metabotropic glutamate receptor 2 (mGluR2) positive allosteric modulator and cysteinyl leukotriene receptor 1 (CysLTR1) antagonist. Eli Lilly was developing LY2300559 for the prevention of migraine. LY2300559 development has been discontinued.
Status:
Investigational
Source:
NCT04636801: Phase 3 Interventional Recruiting Chronic Obstructive Pulmonary Disease
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
CHF6001 is a phosphodiesterase 4 (PDE4) inhibitor optimised for inhaled delivery and tolerability, for the treatment of Asthma and Chronic Obstructive Pulmonary Disease. CHF6001 was 7- and 923-fold more potent than roflumilast and cilomilast, respectively, in inhibiting PDE4 enzymatic activity. CHF6001 inhibited PDE4 isoforms A-D with equal potency, showed an elevated ratio of high-affinity rolipram binding site versus low-affinity rolipram binding site and displayed >20,000-fold selectivity versus PDE4 compared with a panel of phosphodiesterases. CHF6001 effectively inhibited the release of tumor necrosis factor-α from human peripheral blood mononuclear cells, human acute monocytic leukemia cell line macrophages (THP-1), and rodent macrophages (RAW264.7 and NR8383). CHF6001 has the potential to be an effective topical treatment of conditions associated with pulmonary inflammation, including asthma and chronic obstructive pulmonary disease.
Status:
Investigational
Source:
NCT03596762: Phase 2 Interventional Completed Menopause
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT04589845: Phase 2 Interventional Recruiting Solid Tumors
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Idasanutlin (RG-7388) is a second-generation, orally bioavailable, selective p53-MDM2 antagonist. MDM2 is an important negative regulator of the p 53 tumor suppressor and is expressed at high levels in a large proportion of acute myeloid leukemia (AML). Blocking the MDM2-p53 interaction stabilizes p53 and activates p-53 mediated cell death and inhibition cell growth. Idasanutlin is under clinical trial in phase III for treatment AML and in combinations with others drugs in phase I/II for treatment of multiple myeloma.
Status:
Investigational
Source:
NCT03906071: Phase 3 Interventional Active, not recruiting Metastatic Non-Squamous Non-Small Cell Lung Cancer
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Sitravatinib (MGCD516) is a receptor tyrosine kinases (RTK) inhibitor that blocks a wide array of RTKs known to be amplified/overexpressed in sarcomas, which are key regulators of signaling pathways that lead to cell growth, survival and tumor progression. It is involved in driving sarcoma cell growth with IC50 of 3980 nM and is superior to other multi-kinase inhibitors in inhibiting cell proliferation, RTK phosphorylation, and phosphorylation of downstream effectors. The efficacy of sitravatinib was tested using a wide panel of sarcoma cell lines, including malignant peripheral nerve sheath tumor (MPNST), Ewing sarcoma (A673), osteosarcoma (Saos2), and liposarcoma (DDLS, LS141). Both in vitro and in vivo efficacy sitravatinib was significantly better that the other two multi-kinase inhibitors, imatinib and crizotinib. Sitravatinib treatment not only inhibits tumor cell proliferation at low nanomolar concentrations in vitro but also results significant tumor growth suppression in vivo in mouse xenograft models. Sitravatinib is being evaluated in a Phase 1b dose expansion cohort in selected patients with specific genetic alterations that are drivers of tumor growth, with an initial focus on Non-Small-Cell Lung carcinoma (NSCLC) and in other solid tumors where sitravatinib may confer a benefit. Its efficacy and safety is also being tested in Phase II clinical trials in patients with advanced liposarcoma as a monotherapy and NSCLC in combination with nivolumab.
Status:
Investigational
Source:
NCT01121380: Phase 1 Interventional Terminated Healthy
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
BL-1021 was developed by BioLineRx Ltd. for the treatment of neuropathic pain or pain that results from damage to nerve fibers. The drug has completed phase I clinical trials, however further information is not available.
Status:
Investigational
Source:
NCT01265511: Phase 2 Interventional Completed Hepatitis C Infection
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
SCY-635 is a nonimmunosuppressive cyclosporine-based analog that exhibits potent suppression of hepatitis C virus (HCV) replication. SCY-635 has reached the phase II clinical trial for the treatment of patients with hepatitis C Infection. In addition, in the preclinical model, the SCY-635 was studied for the treatment of hepatitis-B in USA.
Status:
Investigational
Source:
NCT04072380: Phase 2 Interventional Completed Narcolepsy
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00542009: Phase 2 Interventional Completed Weight Management
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
CE-326597 is a potent and selective agonist of type 1 cholecystokinin receptor, developed by Pfizer Inc for the treatment of obesity. The physical properties of CE-326597 provided the desired low systemic exposure which was driven by poor absorption of the drug into the intestinal wall. Unfortunately, CE-326597 demonstrated insufficient efficacy for the treatment of either diabetes or obesity after 12 weeks of dosing in Phase 2 clinical trial and was discontinued.
Status:
Investigational
Source:
NCT03055806: Phase 2 Interventional Completed Premature Ejaculation
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
PF-3274167 (Cligosiban) is a potent, selective, brain penetrant oxytocin receptor antagonist. Cligosiban interrupts the expulsion phase of ejaculation by reducing the normal bulbospongiosum burst pattern and reducing the expulsions that accompany bursts. Cligosiban represents a promising compound to test the clinical hypothesis that antagonism of central oxytocin receptors may be of therapeutic benefit in the treatment of premature ejaculation. [11C]PF-3274167 is not a suitable tracer for imaging of OTR in rat brain, probably because of a too low affinity for this receptor in addition to a poor brain penetration. PF-3274167 had been in phase I clinical trial for the treatment of sexual function disorders and urinary incontinence. However, this research has been discontinued.
