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

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Showing 4761 - 4770 of 4933 results

Calcium dobesilate (brand name Doxium) is a veno-tonic drug, which is widely prescribed in more than 60 countries from Europe, Latin America, Asia and the Middle East for three main indications: chronic venous disease, diabetic retinopathy and the symptoms of haemorrhoidal attack. This drugs also in the phase III of clinical trial is an effective adjuvant therapy, with an absence of significant side-effects, in patients with venous ulcers and stasis dermatitis. It was suggested, that the inhibitory effect of calcium dobesilate on platelet function is mediated through the cyclic AMP pathway, and probably through activation of adenyl cyclase.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Rimonabant
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) was an anorectic antiobesity drug that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects. Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first drug approved in that class. There is considerable evidence that the endocannabinoid (endogenous cannabinoid) system plays a significant role in appetitive drive and associated behaviors. It is, therefore, reasonable to hypothesize that the attenuation of the activity of this system would have therapeutic benefit in treating disorders that might have a component of excess appetitive drive or over-activity of the endocannabinoid system, such as obesity, ethanol and other drug abuse, and a variety of central nervous system and other disorders. Data from clinical trials submitted to regulatory authorities showed that rimonabant caused depressive disorders or mood alterations in up to 10% of subjects and suicidal ideation in around 1%, and in Europe, it was contraindicated for people with any psychiatric disorder, including depressed or suicidal people. Additionally, nausea and upper respiratory tract infections were very common (occurring in more than 10% of people) adverse effects; common adverse effects (occurring in between 1% and 10% of people) included gastroenteritis, anxiety, irritability, insomnia and other sleep disorders, hot flushes, diarrhea, vomiting, dry or itchy skin, tendonitis, muscle cramps and spasms, fatigue, flu-like symptoms, and increased risk of falling.
Status:
Possibly Marketed Outside US
Source:
Japan:Trimetazidine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Trimetazidine is a medicine, which is used for the treatment of angina pectoris. The drug mechanism of action is explained by its ability to selectively inhibit long-chain 3-ketoacyl coenzyme A thiolase, an enzyme responsible for mitochondrial beta-oxidation of long chain fatty acids. Trimetazidine also increases pyruvate dehydrogenase activity, binds to the mitochondrial membrane, directly inhibits cardiac fibrosis and improves mechanical resistance of the sarcolemma.
Status:
Possibly Marketed Outside US
Source:
Japan:Minodronic Acid Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Minodronic acid (RECALBON®, Bonoteo®), a third-generation bisphosphonate, was approved in Japan for the oral treatment of osteoporosis. This drug increases the bone mineral density and the strength by inhibiting osteoclastic bone resorption. Nitrogen-containing bisphosphonates, such as minodronic acid (RECALBON®, Bonoteo®) induce osteoclast apoptosis by inhibiting farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate pathway. Inhibition of FPPS in osteoclasts prevents the biosynthesis of isoprenoid lipids that are required for the prenylation of small GTPase signaling proteins necessary for osteoclast function. Similarly, nitrogen-containing bisphosphonates have been shown to inhibit farnesyl pyrophosphate/geranyl pyrophosphate synthase activity.
Status:
Possibly Marketed Outside US
Source:
Canada:ALUMINUM GLUCONATE
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Aluminum gluconate is added to an electrolytic solution for an electrolytic capacitor, the dissolution of aluminum cathode foil caused by high-temperature.
Pimethixene is an antihistamine exerting sedative and antitussive properties. Pimethixene displayed high affinity to serotonin 5-HT2A and 2B, histamine H1 and muscarinic acetylcholine M2 receptors. Oral pimethixene used to calm dry cough and irritation coughs in children.
Status:
Possibly Marketed Outside US
Source:
Japan:Milacainide Tartrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Milacainide (Ro 22-9194) is structurally related to lidocaine and has a pyridine ring in the side chain. Ro 22-9194 is a new Class I antiarrhythmic agent with a TXA, synthase inhibitory activity. In anesthetized, open-chest dogs Ro 22-9194 transiently decreased arterial blood pressure and affected AV conduction more selectively, with a prolongation of the HV interval, than sinoatrial nodal pacemaker activity. In isolated, blood-perfused atria of dogs, Ro 22-9 194 decreased myocardial contractility more than sinoatrial nodal pacemaker activity. Studies in guinea pig papillary muscles and single ventricular myocytes showed that Ro 22-9194 inhibits sodium channels in a use- and voltage-dependent manner, and belongs to the group comprising intermediate kinetic drugs and activated channel blockers. Epinephrine-, digitalis-, two-stage coronary ligation-, and 3-hr coronary ligation-reperfusion-induced ventricular arrhythmias, or aconitine-induced atrial arrhythmias, in dogs were potently suppressed by Ro 22-9194 administered orally or intravenously. In myocardial ischemia and reperfusion-induced arrhythmias of dogs, Ro 22-9194 had an antifibrillatory effect and prevented an increase in venous levels of TXB, released from the ischemic myocardium.
Status:
Possibly Marketed Outside US
Source:
Japan:Incadronate Disodium
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Incadronate (Disodium Cycloheptylaminomethylene diphosphate) is used to treat malignancy-associated hypercalcemia (MAH) in Japan. Experiments on rodents have revealed that this drug could be an effective agent for the treatment of various arthritic conditions, including human rheumatoid arthritis. In addition was shown, that incadronate induced growth inhibition and apoptotic death of pancreatic cancer cells. Incadronate also inhibited migration presumably by preventing the activation of Rho by lysophosphatidic acid. Thus, this drug can be of value in regimens for the treatment of pancreatic cancer.
Status:
Possibly Marketed Outside US
Source:
NCT03376958: Phase 4 Interventional Completed Relapsed and Refractory
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Apatinib is an orally bioavailable, small molecule tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 and used for the treatment of metastatic gastric cancer or gastroesophageal junction cancer that has progressed or relapsed after chemotherapy. To date, second-line ramucirumab and third-line Apatinib are the only anti-angiogenic approaches that have significantly improved the survival of patients with metastatic gastric cancer. Apatinib exhibited potent, highly-selective inhibition of VEGFR-2, c-kit, c-src, and RET tyrosine kinases. The efficacy of Apatinib monotherapy in patients with metastatic gastric cancer or gastroesophageal junction cancer for whom at least two prior chemotherapy regimens had failed was demonstrated in randomized open-label or double-blind phase II trials and a pivotal placebo-controlled phase III trial, all of which were conducted in China. Further clinical experience and long-term pharmacovigilance are required to definitively establish the efficacy and safety profile of Apatinib, including its use in combination with other chemotherapeutic agents.
Setiptiline Maleate is a tetracyclic antidepressant that has been used in the treatment of depression. It has antihistamine and hypnotic–sedative effects, but almost no anticholinergic effects. It is a weak inhibitor of norepinephrine reuptake in vitro and strongly stimulates the release of central norepinephrine by blocking presynaptic α2-adrenoceptors similar to mianserin. It also acts as a 5-HT2A, 5-HT2C, and 5-HT3 receptor antagonist. Unlike most conventional antidepressants, it has no efficacy as a serotonin reuptake inhibitor. It can induce drowsiness and thirst, but it displays low toxicity. Setiptiline Maleate was launched in 1989 for the treatment of depression in Japan.

Showing 4761 - 4770 of 4933 results