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Status:
US Previously Marketed
Source:
EMETE-CON by ROERIG
(1974)
Source URL:
First approved in 1974
Source:
EMETE-CON by ROERIG
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Benzquinamide also known as BZQ; Emete-con, Emetico, is an antiemetic drug, which was discontinued. That drug was used to prevent and treat nausea and vomiting associated with anesthesia and surgery, administered intramuscularly or intravenously. The mechanism of action is not known, but was made predictions which shown, that in spite of benzquinamide did bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR). It was known, that this activity may partially explain the anxiolytic activity effect of the drug. But the dopamine D2 receptor, which by ligand-set similarity resembles α2-AR is an accepted target for emesis. Then benzquinamide was tested towards to the D2, D3, and D4 receptors. Notwithstanding the fact that the α2-AR values are lower than the D2 values, it was predicted, that D2 activity may be the most relevant for emesis.
Status:
US Previously Marketed
Source:
RONDOMYCIN by MEDPOINTE PHARM HLC
(1966)
Source URL:
First approved in 1966
Source:
RONDOMYCIN by MEDPOINTE PHARM HLC
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Methacycline is a tetracycline antibiotic. Similar to other tetracyclines, it has a wide spectrum of antimicrobial action. It is active against most Gram-positive bacteria (pneumococci, streptococci, staphylococci) and Gram-negative bacteria (E. coli, salmonella, shigella, etc.), and towards agents causing onithosis, psittacosis, trachoma, and some Protozoa. Like other tetracyclines, the general usefulness of methacycline has been reduced with the onset of bacterial resistance. Methacycline inhibits the binding of aminoacyl-tRNA to the mRNA-ribosome complex. Methacycline inhibits cell growth by inhibiting translation. It binds to the 16S part of the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. Methacycline is mostly used for the treatment of acute bacterial exacerbations of chronic bronchitis.
Status:
US Previously Marketed
Source:
CHLORPROPAMIDE by PAR PHARM
(1984)
Source URL:
First approved in 1958
Source:
DIABINESE by PFIZER
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Chlorpropamide (DIABINESE®), is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. It appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which chlorpropamide (DIABINESE®) lowers blood glucose during long-term administration has not been clearly established. Extra-pancreatic effects may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs. While chlorpropamide is a sulfonamide derivative, it is devoid of antibacterial activity. Chlorpropamide (DIABINESE®) may also prove effective in controlling certain patients who have experienced primary or secondary failure to other sulfonylurea agent.
Status:
US Previously Marketed
Source:
VIOCIN SULFATE by PFIZER
(1961)
Source URL:
First approved in 1953
Source:
VIOCIN SULFATE by PFIZER
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Viomycin is a basic peptide antibiotic, which is among the most effective agents against multidrug-resistant tuberculosis. The tuberactinomycins, such as Viomycin, target bacterial ribosomes, binding RNA and disrupting bacterial protein biosynthesis. Specifically, viomycin binds to a site on the ribosome which lies at the interface between helix 44 of the small ribosomal subunit and helix 69 of the large ribosomal subunit. The structures of this complexes suggest that the viomycin inhibits translocation by stabilizing the tRNA in the A site in the pretranslocation state.
Status:
Possibly Marketed Outside US
First approved in 2020
Source:
21 CFR 333C
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Dymanthine (Thelmesan) is an Anthelmintic, it is prepared as the hydrochloride and has some activity against hookworm infection, ascariasis, trichuriasis and hymenolepiasis. The drug appears to be safe, well tolerated and to cause few side effects (nausea, vomiting, headache, diarrhea, giddiness).
Status:
Possibly Marketed Outside US
First approved in 2017
Source:
NADA141457
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Capromorelin is a potent ghrelin receptor agonist. Capromorelin is indicated for appetite stimulation in dogs. Plasma insulin-like growth factor-I (IGF-I) was elevated progressively over a 5-d course of daily oral dosing in dogs. In healthy older adults at risk for functional decline, administration of the capromorelin may improve body composition and physical function. Adverse events included fatigue, insomnia, and small increases in fasting glucose, glycosylated hemoglobin, and indices of insulin resistance.
Status:
Possibly Marketed Outside US
First approved in 2016
Source:
NADA141455
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
GALLIPRANT® (grapiprant tablets) is a prostaglandin E2 (PGE2) EP4 receptor antagonist; a non-cyclooxygenase (COX) inhibiting, non-steroidal antiinflammatory drug (NSAID) in the piprant class. Grapiprant is indicated for the control of pain and inflammation associated with osteoarthritis in dogs. It is approved for veterinary use, but it is in phase II development in Japan for the treatment of chronic inflammatory pain, including osteoarthritis and rheumatoid arthritis. Grapiprant shows similar in vitro binding affinity (Ki) for the rat and dog EP4 receptor, 20 and 24 nM, respectively.
Status:
Possibly Marketed Outside US
First approved in 2010
Source:
NADA092444
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Morantel (1,4,5,6-tetrahydro-1-methyl-2-[2-(3-methyl-2-thienyl)ethenyl pyrimidine) is a
tetrahydro-pyrimidine anthelmintic, differing from the related analogue pyrantel by the presence
of a methyl group on the thiophene ring. Morantel tartrate, manufactured by Pfizer, Inc., was approved in the United
States for use in cattle in 1981, and entered the market in early 1982. Three
formulations have been approved in the United States: RUMATEL®
Medicated Premix-88; RUMATEL Cattle Wormer Bolus, and PARATECT
FLEX™ Diffuser, a sustained release bolus. It is intended to treat roundworms and tapeworms. Morantel is
administered in lactating and non lactating cattle as morantel tartrate as a slow-release bolus
(11.8 g morantel base per animal) or as a single oral dose of 6 to 7.5 mg morantel base/kg bw and
in pigs at a single dose equivalent to 7.5 mg base/kg bw. In sheep, the citrate salt is administered
at a single dose equivalent to 5 to 6 mg morantel base/kg bw. Morantel acts as a potent agonist at the acetylcholine receptors on the muscle cells of nematodes.
Activation of the acetylcholine receptors induces a prolonged, spastic paralysis of the worms and
expulsion from the host. It also been reported to block neurotransmission in vertebrates, to
possess nicotine-like properties and to mimic acetylcholine at receptors in autonomic ganglia,
adrenal medullae and respiratory tissues. Morantel and its salts are not used in human medicines.
Status:
Possibly Marketed Outside US
First approved in 2009
Source:
NADA141295
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Toceranib (toceranib phosphate) is an orally bioavailable small molecule inhibitor that blocks a variety of RTKs, including VEGFR2, PDGFRa and KIT. In non-clinical pharmacology studies, toceranib selectively inhibited the tyrosine kinase activity of several members of the split kinase receptor tyrosine kinase (RTK) family, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Toceranib inhibited the activity of Flk-1/KDR tyrosine kinase (vascular endothelial growth factor receptor, VEGFR2), platelet-derived growth factor receptor (PDGFR), and stem cell factor receptor (Kit) in both biochemical and cellular assays. Toceranib has been shown to exert an antiproliferative effect on endothelial cells in vitro. Toceranib treatment can induce cell cycle arrest and subsequent apoptosis in tumor cell lines expressing activating mutations in the split kinase RTK, ckit. Canine mast cell tumor growth is frequently driven by activating mutations in c-kit. Toceranib is a dog-specific anti-cancer drug approved by the U.S. Food and Drug Administration. It is marketed as Palladia as its phosphate salt, toceranib phosphate by Pfizer. PALLADIA (Toceranib) tablets are indicated for the treatment of Patnaik grade II or III, recurrent, cutaneous mast cell tumors with or without regional lymph node involvement in dogs.
Status:
Possibly Marketed Outside US
First approved in 2008
Source:
NADA141285
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cefovecin is a third generation cephalosporin with a broad-spectrum of activity against Gram-positive and Gram-negative bacteria. Cefovecin differs from other cephalosporins in that it is highly protein bound and has a long duration of activity. As with all cephalosporins, the bactericidal action of cefovecin results from the inhibition of bacterial cell wall synthesis through binding to the penicillin-binding proteins (PBPs). It is indicated for the treatment of skin infections secondary superficial pyoderma, abscesses and wounds. Some gastrointestinal adverse effects like vomiting, anorexia or diarrhea were observed.