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Restrict the search for
vitamin a palmitate
to a specific field?
Status:
Investigational
Source:
NCT00002243: Phase 1 Interventional Completed HIV Infections
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Calanolide A is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) originally extracted from a tropical tree (Calophyllum lanigerum) in the Malaysian rain forest. Viral life-cycle studies indicate that calanolide A acts early in the infection process, similar to the known HIV reverse transcriptase (RT) inhibitor 2', 3'-dideoxycytidine. In enzyme inhibition assays, calanolide A potently and selectively inhibits recombinant HIV type 1 RT but not cellular DNA polymerases or HIV type 2 RT within the concentration range tested. Phase I studies have found that calanolide A is well tolerated. Consequently, it has potential clinical applications in combination with other antiviral drugs to suppress HIV-1 mutants. Nevertheless, the development of calanolide A has been delayed due to its low therapeutic index (range: 16–279), non-ideal antiviral activity, and the complexity of its extraction from plants
Status:
Investigational
Source:
NCT01723488: Early Phase 1 Interventional Terminated Alzheimers Disease
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT03176472: Phase 2 Interventional Completed Painful Diabetic Peripheral Neuropathy
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Ricolinostat is a selective inhibitor of HDAC6 with IC50 value of 4.7 nM. Ricolinostat demonstrated good anti-proliferative activity on different cell lines and clinical models of cancer. The drug is being tested in phase I/II for the treatment of multiple myeloma and lymphoid malignancies and in phase I in patients with breast cancer, gynecological cancer, cholangiocarcinoma, recurrent chronic lymphoid leukemia.
Status:
Investigational
Source:
NCT03418714: Phase 1/Phase 2 Interventional Completed Drug Effect
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Salvinorin A has been reported to be the most potent naturally occurring hallucinogen, with an effective dose in humans in the 200- to the 1,000-μg range when smoked; it has been reported to induce an intense hallucinatory experience in humans, with a typical duration of action being several minutes to an hour or so. Salvinorin A is a highly selective agonist of the kappa-opioid receptor (KOR) with few off-target effects. It is a potent and selective dilator of the cerebral vasculature, exhibits rapid penetration through the blood-brain barrier, has potent anti-inflammatory properties, and has the ability to preserve neurovascular unit integrity. As such, salvinorin A is an ideal compound for the prevention and treatment of cerebral vasospasm following subarachnoid hemorrhage.
Status:
Investigational
Source:
NCT02586155: Phase 3 Interventional Completed Diabetes Mellitus, Type 2
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Apabetalone (RVX-208) is a small molecule BET bromodomain inhibitor selective for BRD4-BD2 undergoing clinical development as a potential therapy to enhance ApoA-I production and treat atherosclerosis and prevent cardiovascular disease events. Apabetalone increases apolipoprotein A-I and high-density lipoprotein cholesterol (HDL-Cholesterol) in vitro and in vivo which is believed to provide a new approach to treating atherosclerosis through the stimulation of reverse cholesterol transport. RVX-208 increased the Tm of all BET bromodomains, indicative of binding. RVX-208 competes for acetylated histone H4 peptide binding to both bromodomains of BRD4, similar to JQ-1, but with a preference for BD2 over BD1. RVX-208 also binds to the bromodomains of BRDs 2 and 3 with a similar preference for BD2 (Kd~5–30 nM) over BD1 (Kd~2–3 uM). Treatment of humans for 1 week with oral RVX-208 increased apoA-I, pre-beta-HDL, and HDL functionality. Resverlogix Corp. has commenced a Phase 3 clinical trial in cardiovascular disease patients with type 2 diabetes mellitus with a primary endpoint of time to first occurrence of Major Adverse Cardiac Events (MACE).
Status:
Investigational
Source:
NCT00712829: Phase 1 Interventional Completed Prostate Cancer
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
MIP-1095 I-123 is under investigation in clinical trial phase II to evaluate the safety and efficacy in combination with enzalutamide in patients with prostate-specific membrane antigen (PSMA)-avid metastatic castration-resistant prostate cancer who have progressed on abiraterone. It is known that MIP-1095 potently inhibited the glutamate carboxypeptidase activity of PSMA and when radiolabeled with 123I exhibited high affinity for prostate-specific membrane antigen (PSMA) on human prostate cancer LNCaP cells.
Status:
Investigational
Source:
NCT02560610: Phase 2 Interventional Completed Severe Eosinophilic Asthma
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
OC-459 is a highly potent and selective CRTH2 antagonist which is active on both the recombinant and native human receptor. The Atopix lead compound OC-459 is effective in improving lung function and symptoms in patients with atopic eosinophilic asthma. This group represents 40-50% of all asthmatics and the magnitude of improvement in the responder population is equivalent to high dose inhaled corticosteroids. OC-459 has also been shown to reduce both nasal and eye symptoms in allergic subjects exposed to grass pollen. Of particular interest is the ability of OC-459 to reduce the rate of respiratory infections, an effect related to reduction in Th2 immunity which has a damaging effect on host defence. OC-459 has also demonstrated an excellent safety profile in around 800 subjects exposed drug and no safety issues have been highlighted in long term toxicology. OC-459 is in Phase 2 clinical trial in patients with moderate to severe atopic dermatitis.
Status:
Investigational
Source:
NCT02534350: Phase 2 Interventional Completed Respiratory Syncytial Virus (RSV)
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Presatovir is a novel inhibitor of respiratory syncytial
virus (RSV) fusion F protein patented by Gilead Sciences, Inc. as an antiviral agent. Upon oral administration of GS-5806, this agent specifically binds to F protein on the viral surface, which inhibits RSV F protein-mediated fusion with the host cell membrane and prevents viral entry. This blocks RSV replication, reduces viral load, and decreases the severity of the disease. Presatovir exhibited potent antiviral activity against 75 RSV clinical isolates from both A and B subgroups in vitro. In vivo, presatovir demonstrated efficient penetration into the lung and epithelial lining fluid in Sprague‐Dawley rats and in dogs and cattle. Presatovir demonstrated dose‐dependent antiviral activity in both the upper respiratory tract and the lungs in a nonclinical study of RSV‐infected cotton rats as well as in a clinical study of healthy adults experimentally infected with RSV.
Status:
Investigational
Source:
NCT03292822: Phase 1 Interventional Completed Squamous Cell Carcinoma
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Licochalcone A (LicA) is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch and has a wide spectrum of pharmacological activities such as anti-oxidant, anti-bacterial, anti-viral, and anti-cancer. However, its pharmacological mechanism is not well defined. The anti-Inflammatory effects of LicA on IL-1β-Stimulated human osteoarthritis chondrocytes was reached by activating Nrf2 signaling pathway. LicA showed anti-proliferative and apoptotic effects in breast cancer cells through regulating Sp1 and apoptosis-related proteins in a dose- and a time-dependent manner. In addition, the chemotherapeutic potential of LicA for treatment of human cervical cancer was achieved by inhibition of PI3K/Akt/mTOR signaling.
Status:
Investigational
Source:
NCT01989429: Phase 3 Interventional Completed Plaque Psoriasis
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Pefcalcitol (previously known as M518101), an analog of vitamin D3 (VD3), is an antipsoriatic drug candidate that is designed to achieve much higher pharmacological effects, such as keratinocyte differentiation. This drug is a phosphodiesterase inhibitor and is being developed as a topical ointment formulation. Pefcalcitol was involved in phase III clinical trials in the USA and in Japan in subjects with plaque psoriasis and with palmoplantar keratoderma. In addition, it participated in phase II clinical trial for the warts treatment.
