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Restrict the search for
m ulipristal acetate
to a specific field?
Status:
Investigational
Source:
NCT03016221: Not Applicable Interventional Completed Healthy
(2017)
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Status:
Investigational
Source:
NCT02477020: Phase 2 Interventional Completed Schizophrenia
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
TAK-063 is a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs. TAK-063 is currently being evaluated in clinical trials for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is a cAMP/cGMP phosphodiesterase highly expressed in medium spiny neurons (MSNs) in the striatum. TAK-063 represents a promising drug for the treatment of schizophrenia with potential for superior safety and tolerability profiles.
Status:
Investigational
Source:
NCT02324972: Phase 2 Interventional Completed Atopic Dermatitis
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rosiptor (AQX-1125) is a once daily, orally administered small molecule being developed by Aquinox Pharmaceuticals for the treatment of asthma, bladder pain syndrome/interstitial cystitis (IC/BPS) and chronic prostatitis/chronic pelvic pain syndrome. AQX-1125 is the only clinical-stage, orally administered, SHIP1 activator. AQX-1125 significantly reduces the late response to allergen challenge, with a trend to reduce airway inflammation. AQX-1125 was safe and well tolerated and merits further investigation in inflammatory disorders. AQX-1125 has been used in trials studying the treatment of COPD, atopic dermatitis, interstitial cystitis, and bladder pain syndrome. However, the development has been discontinued.
Status:
Investigational
Source:
NCT03515538: Phase 2 Interventional Completed Oral Mucositis
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
RRX-001, also known as ABDNAZ, is a dinitroazetidine derivative with potential radiosensitizing activity. Upon administration, RRx-001 is able to dilate blood vessels, thereby increasing tumor blood flow and thus improving oxygenation to the tumor site. By increasing oxygen levels, these tumor cells may be more susceptible to radiation therapy. Tumor hypoxia is correlated with tumor aggressiveness, metastasis and resistance to radiotherapy. In mouse models, RRx-001 administered intravenously as a single agent was equipotent to cisplatin while better tolerated. RRx-001 also showed activity as a radiosensitizer in both in vitro and in vivo models. The activity of RRx-001 is thought to be associated with a nucleophilic substitution by circulating thiol compounds and covalent binding of RRx-001 to cysteinyl residues in Hb, followed by the generation of nitrogen oxides. During 2014-2015 EpicentRx has launched Phase 2 trials in brain, colorectal, non-small cell lung, small cell lung and cholangiocarcinoma both alone and in combination. The anti-proliferative effects of RRx-001 are not explainable via a single mechanism. RRx-001 exerts its anti-proliferative effect, at least partially, through interference with glucose 6 phosphate dehydrogenase (G6PD), a key enzyme in the pentose phosphate pathway, responsible for maintaining adequate levels of the major cellular reductant, NADPH.
Status:
Investigational
Source:
NCT01185080: Phase 2 Interventional Completed Allergic Rhinitis
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
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.
Status:
Investigational
Source:
NCT01746979: Phase 3 Interventional Completed Metastatic or Locally Advanced Unresectable Pancreatic Adenocarcinoma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Evofosfamide, also formerly known as TH-302, is an investigational hypoxia-activated prodrug and is used to target cancerous cells under hypoxic conditions, which is a feature possessed by multiple solid tumors including glioblastoma and pancreatic cancer. Within regions of tumor hypoxia, evofosfamide releases bromo isophosphoramide mustard (Br-IPM), a potent DNA alkylating agent that kills tumor cells by forming DNA crosslinks. Once activated in hypoxic tissues, Br-IPM can also diffuse into surrounding oxygenated regions of the tumor and kill cells there via a “bystander effect”. Because of its preferential activation in the targeted hypoxic regions of solid tumors, evofosfamide may be less likely to produce broad systemic toxicity seen with untargeted cytotoxic chemotherapies.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Allocupreide is a copper(l) complex used as an antiinflammatory drug and antiarthritic agent. It was used for the treatment of trigeminal neuralgia.
Status:
Investigational
Source:
NCT03189992: Phase 1 Interventional Unknown status Malignant Tumor of Small Intestine Metastatic to Liver
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Cinobufotalin, the bufadienolide isolated from toad venom,
has displayed antitumor activities in many in vitro systems. It has been shown that cinobufotalin induced significant apoptosis in cultured human lymphoma U-937 cells. It induced DNA fragmentation, mitochondrial membrane
potential decrease, and reactive oxygen species (ROS)
production in U-937 cells. Cinobufotalin induces cytotoxic effect in cultured lung cancer cells. Cinobufotalin (1/5 mg/kg, i.p. twice
daily, for 7 days) significantly inhibited A549 xenograft growth in
mice. Further, same cinobufotalin administration improved mice
survival at week five. Cinobufotalin administration didn’t
significantly affect mice body weight, indicating the relative safety
of this regimen. Thus, cinobufotalin inhibits A549 xenograft
growth in vivo and improves mice survival.
Status:
Investigational
Source:
NCT00302731: Phase 2 Interventional Terminated Menopause
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
