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

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Showing 671 - 680 of 18894 results

Status:
Investigational
Source:
NCT00353067: Phase 3 Interventional Suspended Acute Coronary Syndrome
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Veliflapon (BAY X1005, DG-031) is an enantioselective inhibitor of 5-lipoxygenase activating protein, or FLAP. There are variants in the gene encoding FLAP, and the gene encoding leukotriene A4 hydrolase (LTA4H) linked to risk of heart attack. These variants appear to confer increased risk of heart attack by increasing the production of leukotriene B4 (LTB4), a potent driver of inflammation produced in atherosclerotic plaques. deCODE licensed veliflapon (BAY X1005, DG-031) from Bayer AG, which developed it originally for the treatment of asthma.
Status:
Investigational
Source:
INN:trospectomycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trospectomycin is an aminocyclitol antibiotic similar in structure to spectinomycin. The drug was originally developed by Pharmacia & Upjohn. It is a 6'-propyl analogue of spectinomycin, and lacks the aminosugars in glycosidic linkage which are thought to be responsible for the ototoxicity and nephrotoxicity associated with the aminoglycosides. The mechanism of action of trospectomycin is similar to that of its parent compound, spectinomycin: it binds to the bacterial 30S ribosome and inhibits protein synthesis. The transport mechanism for its delivery to its target site does not appear to be oxygen dependent, and this explains the in-vitro activity of trospectomycin against anaerobic organisms. Trospectomycin has activity against a broad spectrum of pathogenic organisms including Streptococcus, Haemophilus, Gardnerella, Neisseria, Peptococcus, Peptostreptococcus, Bacteroides, Mobiluncus, Chlamydia, Mycoplasma and Ureaplasma spp. Results of in-vivo testing suggest potential utility in a variety of clinical conditions including non-gonococcal urethritis, chlamydial cervicitis, gonorrhoea, pelvic inflammatory disease, pneumonia, anaerobic infections and meningitis. Trospectomycin progressed to late stage clinical trials for treatment of pelvic inflammatory disease (chlamydia) before being abandoned for commercial reasons as the third generation cephalosporins and second generation macrolides in development and use were judged superior at the time.
Status:
Investigational
Source:
INN:denzimol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Denzimol is a new imidazole derivative with anticonvulsant properties. Denzimol suppressed electrically and chemically induced tonic seizures but did not prevent the clonic ones. Denzimol prolongs pentobarbitone sleeping times indicating that drug binds to rat liver microsomes and are potent inhibitors in the rat of mixed function monooxygense activities both in‐vitro and in‐vivo. The antiepileptic activity of the denzimol has been evaluated in patients with poorly controlled partial epilepsy by adding on the drug to the current therapy. Although denzimol increased blood concentrations of carbamazepine, correlation analysis indicated that the improvement was more likely due to intrinsic properties of denzimol. No severe side effects were reported, although several patients experienced nausea and vomiting, which caused 2 patients to drop out. The drug did not show any mutagenic activity when compared with mutagenic standards.
Status:
Investigational
Source:
INN:ciprokiren
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ciprokinen is a renin inhibitor discovered by Roche. Ciprokinen inhibited human renin in a buffer and human plasma with an IC50 of 0.07 and 0.65 nmol/L, respectively. In animal models, acute and chronic administration of ciprokinen lead to a reduction in arterial blood pressure. Development of ciprokinen was discontinued at a preclinical stage.
Status:
Investigational
Source:
INN:idoxifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Idoxifene (also known as CB 7432), a novel selective estrogen receptor modulator, is originally discovered at the CRC Centre for Cancer Therapeutics, Institute. This drug participated in clinical trials phase II in patients with locally advanced/metastatic breast cancer resistant to tamoxifen. In addition, in phase III in postmenopausal women after one year of idoxifene treatment. However, both studies were discontinued because of insufficient effectiveness.
Status:
Investigational
Source:
INN:mibolerone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Mibolerone is a synthetic anabolic steroid. It binds both androgen and progesterone receptors and exerts both androgenic and progestagenic actions. Mibolerone (CHEQUE® Drops) was used in veterinary for estrous (heat) prevention in adult female dogs not intended primarily for breeding purposes. No prescription preparation, human or veterinary, is currently known to contain mibolerone worldwide.
Status:
Investigational
Source:
NCT00137332: Phase 2 Interventional Terminated Arrhythmia
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Rotigaptide (previously known as ZP123) originally was developed by Zealand Pharma as a stable antiarrhythmic peptide analog, which maintains gap junction intercellular communication. Then this drug was licensed to Wyeth Pharmaceuticals where it studied in phase II clinical trials in patients with coronary artery disease and with atrial fibrillation. However, these researches have been discontinued.
Status:
Investigational
Source:
INN:amicycline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Amicycline is an anti-bacterial agent, an antibiotic of tetracycline class.
Status:
Investigational
Source:
NCT01817959: Phase 3 Interventional Completed Islet Transplantation in Diabetes Mellitus Type 1
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Reparixin is a CXC chemokine receptor type 1 (CXCR1) and type 2 (CXCR2) inhibitor. This compound has potential antineoplastic activity. It can be administered orally, binds to CXCR1 (overexpressed on cancer stem cells) and prevents its activation by its ligand interleukin 8. This might result in the death of cancer cells and inhibition of cell progression and metastasis. Reparixin also inhibits CXCR2 activation, possibly reducing both neutrophil recruitment and vascular permeability during inflammation or injury. A phase II clinical trial evaluating the effects of orally administered reparixin on cancer stem cells in the primary tumor and the tumoral microenvironment in an early breast cancer population was terminated. Reparixin has also been suggested as a novel potential therapeutic strategy for aggressive forms of thyroid cancer, based on results of a xenotransplantation study in mice.
Status:
Investigational
Source:
NCT02972658: Phase 3 Interventional Terminated Alzheimer's Disease
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


AZD-3293 camsylate wider known as Lanabecestat camsylate, a salt of Lanabecestat, a drug that was invented for the treatment of Alzheimer's disease. Lanabecestat inhibits beta-secretase 1 cleaving enzyme (BACE1) thus preventing the buildup of beta-amyloid and help stop the progression of Alzheimer's disease. The drug was in phase III clinical trials, but studies were discontinued because of recommendations by an independent data monitoring committee (IDMC). IDMC concluded that all trials, in early Alzheimer’s disease, and in mild Alzheimer’s disease dementia, were not likely to meet their primary endpoints upon completion and therefore should be stopped for futility.