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Status:
Possibly Marketed Outside US
Source:
G 254 300 (ConZip 300 mg)
Source URL:
First approved in 1946
Source:
NDA006035
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
D&C RED NO. 7 is an inactive component of CONZIP®, which is an opioid agonist indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate.
Status:
Possibly Marketed Outside US
Source:
NCT00797589: Phase 4 Interventional Completed Valve Surgery
(2009)
Source URL:
First approved in 1942
Source:
M022
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Malic acid is a tart-tasting organic dicarboxylic acid that contributes to the taste of many sour or tart foods such as apples. Sodium Malate is the sodium salt of Malic Acid. Malic Acid and Sodium Malate can be found in a wide range of cosmetics and personal care products. Sodium Malate functions as a skin conditioning agent-humectant. As a food additive, Sodium Malate has the E number E350. Sodium Malate has demonstrated protective effect on cisplatin-induced toxicity in mice. Sodium malate could become a useful agent for the reduction of CDDP-induced toxicity, particularly nephrotoxicity and hepatotoxicity.
Status:
Possibly Marketed Outside US
Source:
NCT02682524: Phase 4 Interventional Completed Osteoarthritis of Knee
(2015)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Pelubiprofen, 2-[4-(Oxocyclohexylidene methyl)phenyl]propionic acid, is one of the 2-arylpropionic acid class of non-steroidal anti-inflammatory drugs (NSAIDs). It has wide variety of indications proposed: osteoarthritis, rheumatoid arthritis, musculoskeletal pain, post-operative trauma, backache, neck-shoulder syndrome and dental pain. Pelubiprofen is a prodrug of 2-arylpropionic acid with relatively selective effects on cyclooxygenase-2 activity. Antiinflammatory properties of pelubiprofen are due to its ability to both decrease prostaglandin synthesis by inhibiting the activities of cyclooxygenases (COXs) and IkB kinase-b (IKK-b). Pelubiprofen was found to have an anti-edema effect in the carrageenan-induced paw edema model in rats, one of the well-established acute inflammatory models in vivo. Pelubiprofen was well tolerated in single doses up to 120mg and at a dosage of 180 mg/day. No drug accumulation was evident, suggesting that it may be useful for long term treatment.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Zinc dodecyl hydrogen disulphate (Zinc Coco-Sulfate) is a surfactant, cleansing and emulsifying agent. It is used at concentrations from 0.1% to 29%, primarily in soaps, shampoos and toothpastes.
Status:
Possibly Marketed Outside US
Source:
NCT01176318: Phase 4 Interventional Withdrawn Chronic Obstructive Pulmonary Disease
(2010)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Erdosteine is an antioxidant compound developed by Edmond Pharma and approved in Europe for the treatment of chronic bronchitis and COPD. Erdosteine has two thiol groups and is believed to act as a free radicals scavenger (through the formation of the active metabolite I, N-thiodiglycolylhomocysteine). Also the drug effect may be due to the inhibition of the activity of elastase enzyme and its interaction with mucosa. The drug got Orphan Drug designation by FDA for the treatment of bronchiectasis.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Hydroxyresveratrol (Oxyresveratrol) is a major active compound in the heartwood of Artocarpus lacucha. It was first isolated from the heartwood of Artocarpus lakoocha, and has also been found in various plants, including Smilax China, Morus alba, Varatrum nigrum, Scirpus maritinus, and Maclura pomifera. Oxyresveratrol, an aglycone of mulberroside A, has been produced by microbial biotransformation or enzymatic hydrolysis of a glycosylated stilbene mulberroside A, which is one of the major compounds of the roots of M. alba.
Oxyresveratrol plays an important role in anti-tyrosinase, antioxidant, anti-inflammatory, antiviral and neuroprotective properties. There are many A. lacucha commercial products available on the market for skin whitening and anti-aging effects. OxyResvenox™ is the registered trademark of Oxyresveratrol from Sabinsa. Oxyresveratrol is an analog of Resveratrol and is of synthetic origin. The hydroxystilbene compounds including oxyresveratrol and resveratrol showed the potent inhibitory effect on tyrosinase activity. Oxyresveratrol is also naturally present in Morus alba L., Morus bombycis. Oxyresveratrol exhibits a potent inhibitory effect on dopa oxidase activity of tyrosinase
which catalyzes rate-limiting steps of melanin biosynthesis. Oxyresveratrol showed superoxide scavenging effects with the IC50 values 3.81 ± 0.5 uM,
Oxyresveratrol exhibited a DPPH free radical scavenging effect (IC50 = 23.4 ± 1.5 uM).
Oxyresveratrol also showed hepatoprotective effects with EC50 values 32.3 ± 2.62 uM, on
tacrine-induced cytotoxicity in human liver-derived Hep G2 cells. Oxyresveratrol significantly inhibited LPS-evoked nuclear translocation of NF-kappaB and
cyclooxygenase-2 (COX-2) activity in RAW 264.7 cells.
The results suggest that the anti-inflammatory properties of oxyresveratrol might be
correlated with inhibition of the iNOS expression through down-regulation of NF-kappaB
binding activity and significant inhibition of COX-2 activity. Oxyresveratrol revealed a dose-dependent neuroprotective effect in an in vivo stroke model.
This may prove to be beneficial for a therapeutic strategy to limit brain injury in acute brain ischemia.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Bepridil (trade name Vascor) is an amine calcium channel blocker used to treat angina. Bepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride. Bepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes in vitro, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works. Bepridil is no longer sold in the United States, but it is still marketed in other countries. Bepridil has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. Although, it contains one chiral center, it is generally administered as a racemates. The drug bepridil is a racemic mixture of two enantiomers for the 2R as CID 16048570 and 2S as CID 445143. (R)-isomer of bepridil is more active than (-S)- isomer, in certain cases. In the retrogradely perfused, paced rat heart the higher activity was found for the ( )-enantiomer, which
was 4.27 times more potent in increasing coronary flow than the (-)-isomer. The two enantiomers of bepridil showed a lower activity on maximum systolic left ventricular
pressure (MSLVP) than on coronary flow, and a similar 3-4 fold
stereoselectivity with both parameters.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
BI-847325 is a novel, ATP-competitive, orally available inhibitor of Aurora kinases and
MEK. In in vitro studies, BI-847325 inhibited the activity of Xenopus laevis Aurora Kinase
B with an IC50 of 3 nM; with IC50 values for human Aurora kinase A and Aurora kinase C
being 25 and 15 nM, respectively. BI-847325 also inhibited human MEK1 and MEK2 with
respective IC50 values of 25 and 4 nM. BI-847325 had been in phase I clinical trials by Boehringer Ingelheim for the treatment of solid tumours. However, there is no development reported for this study.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Alprenolol is a beta adrenoreceptor blocking agent and 5HT1A antagonist, developed by AstraZeneca and now available as generic drug. It is used for treatment of hypertension, angina pectoris due to coronary atherosclerosis and acute myocardial infarction.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Chlormidazole was the first azole introduced the treatment of topical mycosis. It demonstrated inhibitory activity against many fungi and some gram-positive cocci. It is used for the treatment of fungal and bacterial infections of nails and skin, including interdigital and periungual mycoses. Possible side effects are: local skin irritation, burning, itching.