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Status:
Possibly Marketed Outside US
Source:
NCT04270487: Phase 4 Interventional Completed Irritable Bowel Syndrome
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Otilonium is a musculotropic spasmolytic agent belonging to the family of quaternary ammonium derivatives and successfully used in the treatment of patients affected by Irritable bowel syndrome (IBS) due to its specific pharmacokinetic and pharmacodynamic properties. The positive polarity of the head of the Otilonium molecule determines the main pharmacokinetic property of this drug: a minimal systemic absorption and the consequently high safety profile. Studies on animal models revealed a specific Otilonium accumulation in colonic circular muscle at therapeutic µm concentrations, while its plasma levels were 1000 times lower, together with a poor penetration of the drug in the central nervous system. Consistently, after oral administration to healthy volunteers, the Otilonium plasmatic concentration was very low, less than 1% of the drug was eliminated by urine, and 97% was eliminated by feces. Recent clinical studies showed comparable safety and tolerability for Otilonium and placebo. Otilonium was shown to inhibit the main patterns of human sigmoid motility in vitro, including: the tone of smooth muscle cells (SMCs); the rhythmic phasic contractions induced by the interstitial cells of Cajal; and the strong contractions induced by stimulation of enteric motor neurons mainly by blocking the calcium influx through L-type calcium channels on SMCs. Recent in vitro studies using cultured human colonic SMCs to further assess the musculotropic spasmolytic properties of Otilonium confirmed that this drug causes smooth muscle relaxation through the inhibition of voltage-gated calcium channels (L-type > T-type) and the inhibition of muscarinic and tachykinergic effects.
Status:
Possibly Marketed Outside US
Source:
Lipochol by Carlo Erba
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Thioctic acid amide is a coenzyme, which transfer acetyl and hydrogen in pyruvate deacylation oxidation process, used for pharmaceuticals. Thioctic acid amide has been described as antioxidant, preventing oxidant-mediated apoptosis. It may be used in treatment of insulin resistance by stimulating mitochondrial biogenesis. When used in combination with Alprostadil, it has shown to have a good therapeutic effect on early diabetic nephropathy. Thioctic acid amide is an ingredient of Lipochol, used for prevention of liver diseases, hepatoprotection from drugs, autointoxication.
Status:
Possibly Marketed Outside US
Source:
Pyriproxyfen Virbac by Sumitomo Chemical
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Pyriproxyfen is a broad-spectrum insect growth regulator with insecticidal activity against public health insect pests: houseflies, mosquitoes and
cockroaches. In agriculture and horticulture, pyriproxyfen has registered uses for the control
of scale, whitefly, bollworm, jassids, aphids and cutworms. Pyriproxyfen is used on citrus
fruit in Israel, South Africa, Spain and Italy. Pyriproxyfen is one of several insecticides used
for the control of the red imported fire ant (Solenopsis invicta) in California, USA.
Pyriproxyfen has also been considered by WHO for vector control under its Pesticides
Evaluation Scheme. It is a potent suppressor of embryogenesis and adult formation of the sweetpotato whitefly, Bemisia tabaci (Gennadius), and the greenhouse whitefly, Trialeurodes vaporariorum (Westwood). Dipping of cotton or tomato seedlings infested with 0 to 1-day-old eggs in 0.1 mg litre−1 resulted in over 90% suppression of egg hatch of both B. tabaci and T. vaporariorum. Pyriproxyfen is registered in the U.S. for flea and tick control in the home and on pets, as well as indoor and outdoor ant and roach control. Formulas include carpet powders, foggers, aerosols, shampoos, bait, and pet collars.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Cefroxadine is an antibiotic developed for the treatment of bacterial infectious diseases caused by gram-negative and gram-positive organisms. The information about drug status is unavailable and is supposed to be "discontinued", however it may be manufactured in Italy by Novartis.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Tetragastrin is a C-terminal tetrapeptide (Trp–Met–Asp–Phe–NH2) of gastrin. It is the smallest peptide fragment of gastrin which has the same physiological and pharmacological activity as gastrin. It is used to test the secretion of digestive juice. It causes severe anxiety symptoms when administered to humans and is commonly used in scientific research to induce panic attacks for the purpose of testing new anxiolytic drugs. Tetragastrin is a selective cholecystokinin B (CCKB) receptor agonist. Tetragastrin is used as a gastric stimulant at a dose of 4 ug/kg, it was marketed in Japan under the brand name Gastopsin.
Status:
Possibly Marketed Outside US
Source:
SULINDAC by Fillet, M.|Hubert, P.|Crommen, J.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
(R)-Sulindac is the (R)-enantiomer of nonsteroidal anti-inflammatory drug (NSAID) Sulindac, that is marketed in the U.S. by Merck as Clinoril. Sulindac is a prodrug, derived from sulfinylindene, that is converted in vivo to an active sulfide compound by liver methionine sulfoxide reductases (Msr). The (Msr) family of enzymes includes two major classes, MsrA and MsrB, that specifically reduce the S- and R-epimers of Sulindac. Reduction of (R)-Sulindac to Sulindac Sulfide catalyzed by methionine sulfoxide reductase (Msr)-B. The oxidation of both epimers to sulindac sulfone is catalyzed primarily by the microsomal cytochrome P450 (P450) system. (S)-Sulindac increases the activity of the P450 system better than (R)-sulindac, but both epimers increase primarily the enzymes that oxidize (R)-sulindac. Both epimers can protect normal lung cells against oxidative damage and enhance the killing of lung cancer cells exposed to oxidative stress.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
(S)-Sulindac is the (S)-enantiomer of nonsteroidal anti-inflammatory drug (NSAID) Sulindac, that is marketed in the U.S. by Merck as Clinoril. Sulindac is a prodrug, derived from sulfinyl-indene, that is converted in vivo to an active sulfide compound by liver methionine sulfoxide reductases (Msr). The (Msr) family of enzymes includes two major classes, MsrA and MsrB, that specifically reduce the S- and R-epimers of Sulindac. Reduction of (S)-Sulindac to Sulindac Sulfide catalyzed by methionine sulfoxide reductase (Msr)-A. The oxidation of both epimers to sulindac sulfone is catalyzed primarily by the microsomal cytochrome P450 (P450) system. (S)-Sulindac increases the activity of the P450 system better than (R)-sulindac, but both epimers increase primarily the enzymes that oxidize (R)-sulindac. Both epimers can protect normal lung cells against oxidative damage and enhance the killing of lung cancer cells exposed to oxidative stress.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (MIXED)
Targets:
Conditions:
Flumethrin is a type II synthetic pyrethroid insecticide used externally in veterinary medicine against parasitic insects and ticks on cattle, sheep, goats, horses, and dogs, and the treatment of parasitic mites in honeybee colonies. In veterinary medicine, it is applied topically to sheep, cattle, and goats, as a 1% w/v pour-on or as a plunge dip for the control of ticks, lice, and mites. The pour-on is applied at a rate of 2 mg/kg BW. The plunge dip is diluted at a rate of 1-litre product in 900 liters water. For control of scab, the sheep must be dipped for one minute. Plastic strips impregnated with 3.6 mg Flumethrin are hung in beehives for the diagnosis and treatment of varroatosis in honeybees. Four strips per hive are used for mature colonies and 2 per hive for immature colonies. Flumethrin causes a long-lasting prolongation of the normally transient increase in sodium permeability of the nerve membrane during excitation, resulting in long-lasting trains of repetitive firing. The cyano group on the phenoxy-fluorobenzyl alcohol moiety is considered to be responsible for the long-lasting prolongation of sodium permeability. The type II pyrethroids produce a distinct poisoning syndrome which is characterized by choreoathetosis (sinuous writhing of the whole body) and salvation. Flumethrin on the membrane of nerve cells blocking the closure of the ion gates of the sodium channel during re-polarization. This strongly disrupts the transmission of nervous impulses, causing spontaneous depolarization of the membranes or repetitive discharges. At low concentrations insects and other arthropods suffer from hyperactivity. At high concentrations, they are paralyzed and die. Sensory and nervous cells are particularly sensitive. Flumethrin is a complex mixture of stereoisomers. The molecule contains three asymmetric carbon atoms, there is cis-trans isomerism at the cyclopropane ring and cis-trans isomerism at the carbon-carbon double bond of the alkene. So there are 16 different isomers. Commercial Flumethrin typically contains 92% of the trans isomers on the cyclopropane ring and the cis-configuration at the olefinic carbon-carbon double bond and 8% of the isomer with cis geometry on the cyclopropane ring and the cis-configuration at the olefinic carbon-carbon double bond.
Status:
Possibly Marketed Outside US
Source:
QUINODIS by Kyorin Pharmaceutical
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Fleroxacin is an anti-bacterial agent developed for the treatment of uncomplicated cystitis in women, uncomplicated gonococcal infections, bacterial enteritis, and traveler's diarrea, urinary tract infection, pyelonephritis, skin, soft tissue, bone and joint infections, and lower respiratory tract infections. Fleroxacin acts on bacterials by inhibiting DNA gyrase and topoisomerase IV. Although the current status of the drug in Europe and in the USA is unknown, there is information about its approval and usage in China.
Status:
Possibly Marketed Outside US
Source:
Curaderm BEC5 by Briggs, L.H. et al.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Solasonine, a known glycoalkaloid, is a potential anti-cancer agent. Solasonine is a component of Curaderm BEC5 indicated for the topical treatment of actinic keratosis, keratoacanthoma, basal cell carcinoma and cutaneous superficial squamous cell carcinoma. BEC is a standardized mixture of Solamargine (33%), Solasonine (33%) and di-and monoglycosides of solasodine (34%) extracted from S. sodomaeum, now reclassified as S. linnaeanum. Solasonine could inhibit cell proliferation, migration and colony formation of glioma cells. Treatment of solasonine induced apoptosis via modulating cytochrome c and caspase signaling. Besides, solasonine decreased the expression of proinflammatory mediators and nuclear translocalization of NF-κB p50/p65. Mechanistic investigation further revealed that solasonine may target anti-inflammatory signaling pathway, and more specifically p-p38 and p-JNK MAPKs.