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

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Showing 191 - 200 of 420 results

Status:
Possibly Marketed Outside US
First approved in 2007
Source:
SEMDURAMICIN 150 by Phibro Saude Animal Internacional Ltda
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Semduramicin is an ionophore coccidiostat used in the poultry industry as a feed additive. Semduramicin is marketed under the brand name Aviax among others, indicated for the prevention of coccidiosis in poultry, caused by Eimeria tenella, E. acervulina, E. maxima, E. brunetti, E. necatrix, and E. mitis.
Status:
Possibly Marketed Outside US
Source:
ADVOCIN by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Danofloxacin is a quinolone antibacterial agent for veterinary medicine. The drug is approved by FDA for the treatment of bovine infectious respiratory disease under the name Advocin (mesylate salt). Danofloxacin exerts its action by inhibiting bacterial DNA gyrase.
Status:
Possibly Marketed Outside US
Source:
Canada:SELAMECTIN
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Selamectin (trade name Revolution, Stronghold) is a broad-spectrum endectocide. It is used in dogs and cats for treatment, control and prevention against fleas, heartworms, ear mites, ticks and other parasites. Selamectin is not approved for human use. It is a a semi-synthetic compound of the avermectin class, a macrocyclic lactone.
Status:
Possibly Marketed Outside US
Source:
Dectomax by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Doramectin is a macrocyclic lactone isolated from fermentations of selected strains derived from the soil organism Streptomyces avermitilis. A primary mode of action of macrocyclic lactones is to modulate chloride ion channel activity in the nervous system of nematodes and arthropods. Macrocyclic lactones bind to receptors that increase membrane permeability to chloride ions. This inhibits the electrical activity of nerve cells in nematodes and muscle cells in arthropods and causes paralysis and death of the parasites. Doramectin is indicated for the treatment and control of gastrointestinal roundworms, lungworms, eyeworms, grubs, biting and sucking lice, horn flies, and mange mites in cattle.
Tenidap ([Z]-5-chloro-2,3-dihydro-3-[hydroxy-2-thienylmethylene]-2-oxo-1H-indole-1-carboxamide) is an oxindole derivative, a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory drug candidate that was under development by Pfizer as a promising potential treatment for rheumatoid arthritis. Tenidap shows potent inhibition of cyclooxygenase in vitro, that is of several magnitudes greater than 5-lipoxygenase inhibition. Lipoxygenase inhibition, however, has been difficult to document in vivo because Tenidap is highly protein bound and free drug concentrations are below those necessary for 5-lipoxygenase inhibition. However, several in-vitro activities distinguish Tenidap from conventional cyclooxygenase inhibitors. As shown with stimulated human neutrophils, tenidap inhibits activation of collagenase, lysosomal enzyme secretion, and superoxide generation, as well as aggregation and adhesion to endothelium. Furthermore, unlike Non-steroidal anti-inflammatory drugs (NSAIDs), it lowers circulating C-reactive protein (CRP) concentrations by a magnitude equivalent to hydroxychloroquine and auranofin. This result suggests an effect on the synthesis and/or release of the cytokines known to induce the acute-phase protein response-namely, IL-1, IL-6, and TNF-alpha. Tenidap, like existing second-line drugs, lowers serum IL-6 concentrations, a property not shared by NSAIDs The cytokine inhibitory effect also includes reduced in-vitro concentrations of TNF-alpha and IL-1 from both RA synovium and peripheral blood mononuclear cells. There is no immunosuppressive effect of Tenidap in either animal or clinical studies. In clinical studies. The comparisons between tenidap and other second-line agents show that Tenidap produced a faster reduction in CRP than Auranofin. The rate of withdrawal because of inefficacy was similar (18-20%) in Auranofin and Tenidap groups. The quality of life using the arthritis impact measurement scales has also been assessed Scores were better with tenidap than with NSAID monotherapy, but equivalent to the second line plus NSAID combinations. Tenidap is registered in the United States, Netherlands, and Italy but is not marketed because marketing approval was rejected by the FDA in 1996 due to liver and kidney toxicity, which was attributed to metabolites of the drug with a thiophene moiety that caused oxidative damage.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Trimazosin was originated by Pfizer and was licensed to Bristol-Myers Squibb worldwide except for Canada, Mexico and the USA. Trimazosin is a quinazoline antihypertensive agent structurally related to the selective alpha 1-adrenoceptor blocker prazosin. Trimazosin is an alpha adrenergic receptor antagonist. Compared with prazosin, trimazosin was a less potent but more efficacious hypotensive agent. At doses which caused equal or even greater hypotensive effects than those caused by prazosin, trimazosin caused less inhibition of pressor responses to phenylephrine. When administered during a maximum hypotensive response to prazosin, trimazosin caused an additional fall in pressure. Trimazosin is an effective antihypertensive when given by itself or in combination with a diuretic. Its ability to induce vasodilation without concomitant sodium retention or stimulation of the renin axis may be an important factor in its effectiveness. Trimazosin has the potential to cause sustained improvement in left ventricular function, both at rest and during exercise, in patients with chronic congestive heart failure (CHF).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Zopolrestat is a novel carboxylic acid aldose reductase inhibitor. It has been shown to normalize sorbitol, fructose, and myoinositol levels in sciatic nerve, lens, retina, and kidney in diabetic rats and to restore normal renal plasma flow in galactosemic rats. It is being evaluated as an aldose reductase inhibitor for the treatment of diabetic complications.
Status:
Possibly Marketed Outside US
Source:
APOQUEL by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Oclacitinib (PF03394197) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. Oclacitinib inhibited JAK family members by 50% at concentrations (IC50 's) ranging from 10 to 99 nM and did not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nm). Oclacitinib was most potent at inhibiting JAK1 (IC50 = 10 nm). Oclacitinib also inhibited the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50 's ranging from 36 to 249 nM. Oclacitinib as oclacitinib maleate is approved for control of pruritus associated with allergic dermatitis and control of atopic dermatitis in dogs at least 12 months of age.
Sultamicillin is the mutual prodrug of sulbactam and ampicillin. It is the tosylate salt of the double ester of sulbactam plus ampicillin. Sulbactam is a semisynthetic ß-lactamase inhibitor which, in combination with ampicillin, extends the antibacterial activity of the latter to include some ß-lactamase-producing strains of bacteria that would otherwise be resistant. The combination of sulbactam plus ampicillin for parenteral use has previously been shown to be clinically and bacteriologically effective in a variety of infections. Sultamicillin is marketed under a trade name Unasyn among others.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fluperolone (P-1742 or Methral) is a topical fluorinated prednisolone derivative exerting an anti-inflammatory activity. It demonstrated effectivity in the treatment of various dermatoses.

Showing 191 - 200 of 420 results