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Restrict the search for
angiotensin ii
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Argimesna (also known as arginine 2-mercaptoethanesulfonate) is a sulfhydryl group-containing molecule, which has no effect on glutathione status or on the total thiol pool, but is an uroprotective agent. Argimesna was investigated for the prevention of haemorrhagic cystitis from ifosfamide (IFO), but these studies were discontinued
Class (Stereo):
CHEMICAL (ACHIRAL)
Ripisartan (UP-269-6) is a specific nonpeptide angiotensin II receptor antagonist. Oral administration of ripisartan in rats and dogs resulted in a dose-dependent and long-lasting inhibition of the angiotensin II-induced pressor response. It did not show agonistic properties in animals. In vitro, ripisartan was found to bind selectively to AT1 receptors. In humans, it showed high biliary excretion and reabsorption. Canine studies have suggested it might have cardioprotective properties after acute ischemia-reperfusion.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Piclamilast (RP 73401), is a selective PDE4 inhibitor. It is comparable to other PDE4 inhibitors for its anti-inflammatory effects. It has been investigated for its applications to the treatment of conditions such as asthma, dermatitis, rheumatoid arthritis. Emesis is the most commonly cited side effect of piclamilast.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Iganidipin is a new dihydropiridynic derivative of calcium antagonist. It is the only currently available calcium antagonist in the form of ophthalmic solution. Its topical administration increases ipsilateral optic nerve head blood flow in rabbits and monkeys and inhibits the contraction of blood vessels induced by endothelin -1. Iganidipin is also used for treat Angina pectoris and Hypertension.
Status:
Investigational
Source:
NCT00820560: Phase 1 Interventional Completed Solid Tumors and Hematologic Malignancy
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Aderbasib, also known as INCB007839, is an orally bioavailable low nanomolar hydroxamate-based inhibitor of the ADAM (A Disintegrin And Metalloprotease) family of multifunctional membrane-bound proteins with potential antineoplastic activity. Aderbasib represses the metalloproteinase "sheddase" activities of ADAM10 and ADAM17, which may result in the inhibition of tumor cell proliferation.
In preclinical studies, Aderbasib with lapatinib prevented the growth of HER-2/neu–positive BT474-SC1 human breast cancer xenografts in vivo. Aderbasib was being developed by Incyte as a potential adjunctive treatment for metastatic breast cancer. Aderbasib in combination with trastuzumab increased the response rate in HER2 positive metastatic breast cancer patients with advanced disease, relative to historical controls (50% versus 15–35%). INC7839 also improved progression-free survival in a subset of the patients expressing the p95 fragment of HER2. Aderbasib development was halted in 2011 after positive findings from Phase II trials were contradicted by further research. Aderbasib is currently being tested in combination with rituximab for diffuse large B cell non-Hodgkin lymphoma.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Osanetant (SR-142801) is a NK3 receptor antagonist, it has a higher affinity for human and guinea pig NK3 receptors than for rat NK3 receptors. Osanetant was under development for the treatment of schizophrenia and other Central Nervous System (CNS) disorders. It was developed by Sanofi-Aventis (formerly Sanofi-Synthelabo). Sanofi was originally investigating its potential use as a treatment for psychosis and anxiety. Following phase IIa clinical trials, osanetant entered phase IIb development in February 2001. In a review of its R&D portfolio, the company announced in August 2005 that it would cease any further development of osanetant. This follows an earlier decision to discontinue development of eplivanserin for schizophrenia.
Status:
Investigational
Source:
NCT03284385: Phase 2 Interventional Active, not recruiting Clear Cell Renal Cell Carcinoma
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
AZD1775 selectively targets and inhibits WEE1, a tyrosine kinase that phosphorylates cyclin-dependent kinase 1 (CDK1, CDC2) to inactivate the CDC2/cyclin B complex. Inhibition of WEE1 activity prevents the phosphorylation of CDC2 and impairs the G2 DNA damage checkpoint. This may lead to apoptosis upon treatment with DNA damaging chemotherapeutic agents. Current ongoing trials of AZD1775 include monotherapy and combination therapy with certain DNA damaging agents in solid tumors, ovarian tumors, gynaecological cancer, non-small cell lung cancer. AZD1775 is genotoxic, which is considered to be a result of its mechanism of action. Common serious adverse events (with chemotherapy) include: febrile neutropenia, neutropenia, thrombocytopenia.
Status:
Investigational
Source:
NCT00003523: Phase 2 Interventional Completed Ovarian Cancer
(1999)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Rubitecan [Orathecin™] is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral compound being developed for the treatment of pancreatic cancer and other solid tumours by SuperGen. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Netoglitazone (also called MCC-555) is a hypoglycemic agent belonging to the thiazolidinedione group that exerts both peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist activity. It was developed by Mitsubishi-Tokyo (formerly Mitsubishi Chemical) as a potential treatment for type 2 diabetes due to the enhancement of insulin sensitivity. This drug was in clinical trial phase II but then was discontinued. In addition, was also investigated the behaviour of MCC-555 on colorectal cancer (CRC) cells and was revealed, that the drug had an effect on the early events of colon carcinogenesis and could be a potential preventive compound for CRC.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Atizoram (CP-80633) is a phosphodiesterase IV inhibitor with bronchodilatory and antiinflammatory properties. It was in phase II trials with Pfizer in the US for the treatment of asthma, atopic dermatitis and psoriasis. Development of atizoram has been discontinued in the asthma indication and no recent development has been reported for the other indications. CP-80633 inhibits PDE4 isozymes (human lung IC50 = 1.27 uM) in the absence of effects on PDE1, PDE2, PDE3 and PDE5 isozymes (IC50 > 100 uM). It exhibits no significant selectivity for any single cloned PDE4A, B, C or D isoform.
