U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 691 - 700 of 4227 results

Status:
Investigational
Source:
USAN:OCTICIZER [USAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Octicizer is used as a plasticizer.
THIOINOSINE (Methylmercaptopurine riboside, NSC- 40774) is a purine derivative with antineoplastic and anti-angiogenic properties. THIOINOSINE is readily converted in cells to its active form, 6-methylmercaptopurine ribonucleoside 5'- monophosphate (MMPR-P), by the enzyme adenosine kinase. THIOINOSINE inhibits amidophosphoribosyltransferase, the first committed step in de novo purine synthesis, and inhibits fibroblast growth factor-2 (FGF2)-induced cell proliferation. It has been used similarly to Mercaptopurine in the treatment of Leukemia. It has being tested in clinical trials for advanced pancreatic cancer.
Status:
Investigational
Source:
NCT04009044: Phase 2 Interventional Recruiting Cancer Survivor
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hydroxytamoxifen (Afimoxifene) is an active metabolite of tamoxifen exerting estrogen receptor modulatory function. In addition, hydroxytamoxifen binds to regulates transcriptional activity of the estrogen-related receptor gamma. ASCEND Therapeutics, Inc. was developing TamoGel (4-hydroxytamoxifen gel) for a variety of estrogen-dependent conditions, including breast cancer, cyclic breast pain and gynecomastia.
Apilimod is a small molecule inhibitor of interleukin-12 and interleukin-23 synthesis thereby preventing IL-12/IL-23 mediated immune responses. Apilimod is also observed to inhibit the nuclear accumulation of NF-kappB protein family, and viral infections dependent on phosphatidylinositol-3-phosphate 5-kinase (PIKfyve). Apilimod has been investigated as a potential treatment for a number of autoimmune conditions.
Status:
Investigational
Source:
INN:belaperidone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Belaperidone (LU111995) is a recently identified antipsychotic agent with high 5-hydroxytryptamine2 and dopamine D4 receptor affinities as well as D4 versus D2 receptor selectivity. The drug did not produce catalepsy. LU111995 prolongs the Q-T interval to a limited degree and is not arrhythmogenic over the physiological range of cycle lengths. Belaperidone had been in phase II clinical trials for the treatment of schizophrenia. However, the study about this drug candidate was discontinued.
Status:
Investigational
Source:
USAN:Asulacrine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Asulacrine, also known as CI-921, an inhibitor of topoisomerase II, participated in clinical trials phase II for the treatment of cancer. In spite of the positive and promising results, this drug showed the toxicity, phlebitis that blocks its implementation in the future.
Status:
Investigational
Source:
NCT00663429: Phase 2 Interventional Completed Neuroendocrine Carcinoma
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Atiprimod is an oral azaspirane which was initially developed by Smith Kline and French Laboratories for treating rheumatoid arthritis (discontinued in phase I). Due to its anti-inflammatory, antineoplastic, and antiangiogenic properties, the drug was tested in patients with Neuroendocrine Carcinoma and Multiple Myeloma and reached phase II (discontinued). In vitro studies revealed that atiprimod exerts its action by inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.
Status:
Investigational
Source:
NCT00646958: Phase 2 Interventional Completed Infectious Skin Diseases
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Radezolid (RX-1741) is a novel oxazolidinone antibiotic agent and is the first biaryloxazolidinone in clinical development. It is being developed by Rib-X Pharmaceuticals, Inc. for the treatment of serious multi-drug–resistant infections. Radezolid has completed two phase-II clinical trialsfor the treatment of community-acquired pneumonia; uncomplicated skin and skin structure infections. The mechanism of action for this drug seems to be an inhibition of 50S ribosomal subunit.
Status:
Investigational
Source:
INN:milfasartan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Milfasartan is an inhibitor of angiotensin II receptor type 1 was used in phase II clinical trial for the treatment of hypertension. However, these studies were discontinued.
Status:
Investigational
Source:
NCT01064037: Phase 2 Interventional Terminated Heart Failure
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Cinaciguat acts specifically on oxidized/haem-free soluble guanylyl cyclase by binding to the enzyme's haem pocket and mimicking the nitric-oxide-bound haem group. It is in clinical development for the treatment of acute decompensated heart failure. Cinaciguat had been in phase II clinical trials. However, trials were terminated early because of an excess of hypotension in the cinaciguat arms and subsequent slow enrolment.