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

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Showing 331 - 340 of 665 results

Suplatast is a novel immunomodulator that can adjust the imbalance in the Th1/Th2 immune response and shows clear clinical efficacy against bronchial asthma (BA). Suplatast tosilate helps to suppress the production of IgE, to block the production of cytokines and to suppress allergy-related eosinophils. Clinical studies on the efficacy of Suplatast were carried out in Japan. Suplatast showed adequate efficacy for the treatment of BA, allergic rhinitis and atopic dermatitis. Suplatast is now available for the management of BA as a controller of the Th2-dependent allergic inflammation. Suplatast tosilate is not approved in the United States, but is available in Japan as Tosilart® and IPD Capsules®. IPD-1151T (suplatast tosilate) was originated by Taiho and is being developed for the treatment of interstitial cystitis and chronic non-bacterial prostatitis as additional indications. IPD-1151T treatment for 1 year resulted in a significantly increased bladder capacity and decreased symptoms, such as urinary urgency, frequency and lower abdominal pain, in patients with nonulcerative interstitial cystitis.
Status:
Possibly Marketed Outside US
Source:
Japan:Propentofylline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Propentofylline is a selective inhibitor of adenosine transport and phosphodiesterase. For several years it has been well established in the geriatric therapy of the dog improving hemodynamics in cerebral and peripheral compartments. In human medicine clinical development of this pharmaceutical has already entered an advanced stage for the long-term therapy of patients with Alzheimer's disease and vascular dementia. In the brains of senile dogs and in human patients suffering from Alzheimer's disease comparable neuropathological findings can be made. In experimental models of vascular dementia and/or Alzheimer's disease it improves cognitive functions, inhibits inflammatory processes as well as excessive activation of microglia, formation of free radicals, cytocines and abnormal amyloid precursor proteins (APP). It stimulates synthesis and liberation of nerve growth factor (NGF) and reduces ischemic damage to the brain. In clinical studies in humans it improved cognitive functions as well as global functions and the ability to cope with tasks of routine daily life in patients suffering from Alzheimer's disease and vascular dementia. Possible mechanisms of action include a direct glial modulation to decrease a reactive phenotype, decrease glial production and release of damaging proinflammatory factors, and enhancement of astrocyte-mediated glutamate clearance. Net effects of propentofylline in vivo will be dependent on the concentrations of propentofylline and adenosine available and on the subtypes of adenosine receptors, phosphodiesterases, and nucleoside transporters present. In March, 2000 Aventis Pharma, announced that was discontinuing development of propentofylline as a possible treatment for Alzheimer's disease. The decision was a result of the company's portfolio review process which is intended to ensure that resources are devoted only to projects with a high potential for success.
AL3818 (anlotinib) is a receptor tyrosine kinase inhibitor targeting vascular endothelial growth factor receptors (VEGFR1, VEGFR2/KDR, and VEGFR3), stem cell factor receptor (C-kit), platelet-derived growth factor (PDGFβ), and fibroblast growth factor receptors (FGFR1, FGFR2, and FGFR3). Anlotibib is a kind of innovative medicines approved by State Food and Drug Administration(SFDA:2011L00661) which was researched by Jiangsu Chia-tai Tianqing Pharmaceutical Co., Ltd. Phase III development is underway for the treatment of thyroid cancer, gastric cancer, leiomyosarcoma; non-small cell lung cancer; synovial sarcoma; thyroid cancer etc.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Rociletinib is a novel, potent, small molecule, third generation TKI that irreversibly binds and inhibits EGFR with the common activating (L858R, Del19) and T790M resistance mutations. The proposed indication of rociletinib is for the treatment of patients with mutant EGFR NSCLC who have been previously treated with an EGFR-targeted therapy and have the T790M mutation as detected by an FDA approved test. The results from two Phase 2 studies show that rociletinib 625 mg BID treatment has a favorable benefit:risk profile in patients with recurrent T790M-positive mutant EGFR NSCLC based on clinically meaningful and durable responses and a well-established and acceptable safety profile in this patient population with terminal lung cancer. In May 2016, Clovis Oncology, Inc. announced it has terminated enrollment in all ongoing sponsored studies of rociletinib, including TIGER-3, after the company was notified at meeting with the FDA that it could anticipate receiving a Complete Response Letter (CRL) for the rociletinib NDA on or before the PDUFA date of June 28, 2016. Clovis has also withdrawn its Marketing Authorization Application of rociletinib with European regulatory authorities.
Status:
Possibly Marketed Outside US
Source:
Japan:Mepranoprofen Arbamel
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



N,N-Dimethylcarbamoylmethyl alpha,2-dimethyl-5H-[1]- benzopyrano[2,3-b]pyridine-7-acetate (Y-23023/ Tilnoprofen arbamel) is a prodrug developed as a new non-steroidal anti-inflammatory drug (NSAID), by Yoshitomi and Japan Tobacco for treatment pain in Rheumatoid arthritis, but was discontinued. Y-23023 is rapidly hydrolysed to an active metabolite, alpha,2-dimethyl-5H-[1]benzopyrano[2,3-b]pyridine-7-acetic acid (TILNOPROFENIC ACID), cyclo-oxygenase inhibitor.
Solithromycin is a highly potent next-generation macrolide, the first fluoroketolide, which has potent activity against most macrolide-resistant strains. In vitro and in vivo studies have shown potent activity against S. pneumoniae as well as an extended spectrum of activity against CA-MRSA, enterococci, Mycobacterium avium and in animal models of malaria. It is also active against atypical bacteria, such as Legionella, Chlamydophila, Chlamydia, Mycoplasmaand Ureaplasma and against gonococci and other organisms that cause genitourinary tract infections. It is 8-16 times more potent than azithromycin and is active against azithromycin-resistant strains. Its activity against resistant strains is driven by its ability to bind to three sites on the bacterial ribosome, compared to one or two for current macrolides. It binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis. The binding to three ribosomal sites is expected to limit resistance development. On July 2016 Cempra Announces FDA Acceptance of IV and oral formulations of Solithera (solithromycin) New Drug Applications for in the treatment of community-acquired bacterial pneumonia.
Status:
Possibly Marketed Outside US
Source:
Zaldaride maleate by Ciba-Geigy (Novartis)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Zaldaride is a calmodulin antagonist known to produce inhibition of calmodulin-dependent voltage-gated ion channels including those of Ca2 , Na , and K . Zaldaride was also observed to inhibit nicotinic acetylcholine receptor (nAChR) channel currents. Zaldaride has been studied in clinical trials as a potential treatment for travelers diarrhea.
Besipirdine is a potential novel first-in-class oral treatment for over active bladder currently in Phase II development, with a mechanism of action clearly different from that of antimuscarinics. It was under evaluation by Aventis up to phase III for Alzheimer’s disease, involving the administration of the compound to over 1500 patients. However, this research has been discontinued. Besipirdine antagonizes alpha-2 and alpha-1 adrenoceptors and inhibits both norepinephrine and serotonin uptake. The most common adverse events were asymptomatic postural hypotension and asymptomatic bradycardia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. Tasosartan is infrequently in the treatment of hypertension and heart failure. The manufacturer withdrew it from FDA review after phase III clinical trials showed elevated transaminases. Tasosartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Tasosartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance.
Status:
Possibly Marketed Outside US
Source:
Japan:Mitobronitol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Mitobronitol (1,6-dibromo-1,6-dideoxy-D-mannitol, Dibromomannitol) is a brominated analog of mannitol, it is one of a number of carbohydrate derivatives which have exhibited varying degrees of antineoplastic activity. Hungarian investigators first synthesized a series of cytostatic carbohydrate derivatives over two decades ago. Dibromomannitol (DBM) and its conformational isomer dibromodulcitol (DBD) have undergone extensive clinical investigation in the United States. DBD differs from its conformational isomer DBM in activity spectrum, having significant activity against solid tumors and its relative lack of nephrotoxicity. Clinical trials with DBM in the U.S. were carried out mainly in CML; the trials were based on foreign reports of activity in this tumor type. Only the oral form was available for clinical use.

Showing 331 - 340 of 665 results