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Restrict the search for
vitamin a palmitate
to a specific field?
Status:
Investigational
Source:
INN:brezivaptan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT03563599: Phase 2 Interventional Completed Treatment-naïve, Sputum Smear-positive Patients With Drug-sensitive Pulmonary TB
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Q203 (6-chloro-2-ethyl-N-(4-(4-(4-(trifluoromethoxy)phenyl)piperidin-1-yl)benzyl)imidazo [1,2-a]pyridine-3-carboxamide) is an an imidazopyridine antitubercular
compound. Q203 targets the cytochrome b subunit (QcrB) of the cytochrome bc1 complex. This complex is an essential component of the respiratory electron transport chain of ATP synthesis. Q203 inhibited the growth of multidrug-resistant (MDR) and extensively drug-resistant (XDR) M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range and was efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight, which highlights the potency of this compound. In addition, Q203 displays pharmacokinetic and safety profiles compatible with once-daily dosing. Q203 is a promising new clinical candidate for the treatment of tuberculosis.
Status:
Investigational
Source:
NCT02457793: Phase 1 Interventional Completed Non-Small Cell Lung Cancer, Metastatic Colorectal Cancer, Metastatic Non Small Cell Lung Cancer, Metastatic Cancers, Melanoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
GDC-0994 (RG7842) is a selective inhibitor of ERK1/2, also known as extracellular-signal-regulated kinases. Daily, oral dosing of GDC-0994 results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. GDC-0994 neither increases nor decreases phospho-ERK, suggesting that different ERK inhibitors have alternative mechanisms of action with respect to feedback signaling. GDC-0994 is currently advancing in a Phase 1 trial in patients with solid tumors.
Status:
Investigational
Source:
NCT01631383: Phase 1 Interventional Completed Cocaine Use
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tetrahydropalmatine is a tetrahydroprotoberberine isoquinoline alkaloid that is a primary active constituent of herbal preparations containing plant species of the genera Stephania and Corydalis. The levo isomer of THP (L-THP) appears to contribute to many of the therapeutic effects of these preparations. The pharmacological profile of L-THP, which includes antagonism of dopamine D1 and D2 receptors and actions at dopamine D3, suggests that it may have utility for treating addiction. Clinical trials where L-THP was used for the treatment of cocaine and heroin addiction have promising results. The clinical trial is planned for the treatment of schizophrenia. L-Tetrahydropalmatine is recorded in the Chinese pharmacopoeia.
Status:
Investigational
Source:
NCT04123379: Phase 2 Interventional Active, not recruiting Non-small Cell Lung Cancer
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT03605849: Phase 3 Interventional Completed Attention Deficit Disorder
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Centanafadine is an oral triple reuptake inhibitor that has been developed by DOV Pharmaceutical as a treatment for attention-deficit hyperactivity disorder (ADHD). Centanafadine works by modulating the activity of norepinephrine, dopamine, and serotonin, three neurotransmitters known to be relevant in patients with ADHD. In the human abuse liability study, immediate-release centanafadine demonstrated a reduced abuse potential compared with the schedule II stimulants d-amphetamine and lisdexamfetamine. Treatment with high doses of immediate-release centanafadine resulted in a markedly different profile than that of the comparators, with most subjects experiencing the acute onset of adverse effects, including nausea, vomiting, and dysphoria. Almost 2 hours after the administration of centanafadine, the test subjects reported “liking” at about two-thirds of the magnitude of amphetamines, a finding that may have indicated dopamine activity. However, unlike amphetamines, which provided an immediate positive experience, the subjects receiving centanafadine experienced negative effects before reaching that point.
Status:
Investigational
Source:
NCT03908242: Phase 1 Interventional Unknown status Diabetes
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Status:
Investigational
Source:
NCT04586023: Phase 3 Interventional Active, not recruiting Relapsing Multiple Sclerosis
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
G-0853 (also GDC-0853, or Fenebrutinib) is a potent, selective, orally administered, and noncovalent Bruton's tyrosine kinase (Btk) inhibitor currently in clinical development. Upon administration, G-0853 inhibits the activity of Btk and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and Btk-mediated activation of downstream survival pathways, which leads to the inhibition of the growth of malignant B-cells that overexpress BTK. BTK is overexpressed in B-cell malignancies, and plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival. G-0853 suppresses B cell- and myeloid cell-mediated components of disease and demonstrates dose-dependent activity in an in vivo rat model of inflammatory arthritis. G-0853 demonstrates highly favorable safety, pharmacokinetic (PK), and pharmacodynamic (PD) profiles in preclinical and Phase 2 studies ongoing in patients with rheumatoid arthritis, lupus, and chronic spontaneous urticaria.
Status:
Investigational
Source:
Cancer. Jan 1998;82(2):292-300.: Phase 2 Human clinical trial Completed Lung Neoplasms
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Echinomycin is a cyclic peptide of the family of quinoxaline antibiotics that was originally isolated from Streptomyces echinatus. It is thought to act as a bifunctional DNA intercalator. Echinomycin has a binding site size of four base pairs. The strong binding sites for echinomycin contain the central two-base-pair sequence 5'-CG-3'. Echinomycin interferes with HIF-1 DNA binding in a sequence-specific fashion. It was brought into clinical trials by the NCI 20 years ago based on its antitumor activity. It has been extensively tested in phase I-II clinical trials. Nausea, vomiting, reversible liver enzyme abnormalities, and allergic reactions were the most common toxicities encountered. However, minimal or no antitumor activity was found in phase II clinical trials.
Status:
Investigational
Source:
NCT04533529: Phase 3 Interventional Completed Depressive Disorder, Major
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
2-(4,6-DIMETHYLPYRIMIDIN-2-YL)-5-((2-FLUORO-6-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)CARBONYL)OCTAHYDROPYRROLO(3,4-C)PYRROLE (Seltorexant, MIN 202), a small molecule, selective orexin receptor type-2 antagonist, is being developed by Minerva Neurosciences and Janssen Research & Development for the treatment of insomnia and major depressive disorder. Seltorexant has shown high in vitro affinity
(affinity pKi =8.0 and 6.1 for OX2R and OX1R respectively) for the
human OX2R and approximates two logs selectivity ratio versus
its affinity for the OX1R. Seltorexant demonstrated a dose-dependent normalization of sleep and a trend towards improvement of subjective depressive symptoms in antidepressant-treated MDD
patients with residual insomnia. Additionally, seltorexant’s
favorable PK profile as a potential sedative-hypnotic drug was
confirmed in a MDD population and did not demonstrate unacceptable adverse events or unwanted next-day CNS effects. Seltorexant is in phase II clinical trials for both insomnia and MDD.
