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Status:
US Previously Marketed
Source:
POTIGA by GLAXOSMITHKLINE
(2011)
Source URL:
First approved in 2011
Source:
POTIGA by GLAXOSMITHKLINE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Ezogabine (U.S. adopted name) or retigabine (international nonproprietary name) is one of a family of aminopyrroles with anticonvulsant activity. It is used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients. The drug was approved by the European Medicines Agency under the trade name Trobalt and by the United States Food and Drug Administration (FDA), under the trade name Potiga. The mechanism by which ezogabine exerts its therapeutic effects has not been fully elucidated. In vitro studies indicate that ezogabine enhances transmembrane potassium currents mediated by the KCNQ (Kv7.2 to 7.5) family of ion channels. By activating KCNQ channels, ezogabine is thought to stabilize the resting membrane potential and reduce brain excitability. This mechanism of action is unique among antiepileptic drugs, and may hold promise for the treatment of other neurologic conditions, including migraine, tinnitus and neuropathic pain. In vitro studies suggest that ezogabine may also exert therapeutic effects through augmentation of GABA-mediated currents.
Status:
US Previously Marketed
Source:
VICTRELIS by MERCK SHARP DOHME
(2011)
Source URL:
First approved in 2011
Source:
VICTRELIS by MERCK SHARP DOHME
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Conditions:
Boceprevir (trade name Victrelis) is first-generation, selective, small molecule inhibitor of the non-structural serine protease (NS3) and NS4A polypeptide complex (NS3/NS4A) and is a direct acting antiviral drug against the hepatitis C virus. It is indicated the treatment of chronic hepatitis C (CHC) genotype 1 infection, in combination with peginterferon alfa and ribavirin, in adult patients (18 years of age and older) with compensated liver disease, including cirrhosis, who are previously untreated or who have failed previous interferon and ribavirin therapy. Boceprevir is not approved as a monotherapy. Upon administration, boceprevir reversibly binds to the active center of the HCV NS3/NS4A and prevents NS3/NS4A protease-mediated polyprotein maturation. This disrupts the processing of viral proteins and the formation of a viral replication complex, which inhibits viral replication in HCV genotrype 1-infected host cells. NS3, a serine protease, is essential for the proteolytic cleavages within the HCV polyprotein and plays a key role during HCV viral RNA replication. NS4A is an activating factor for NS3.
Status:
US Previously Marketed
Source:
ARCAPTA NEOHALER by NOVARTIS
(2011)
Source URL:
First approved in 2011
Source:
ARCAPTA NEOHALER by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Indacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by Novartis. It was approved by the European Medicines Agency (EMA) under the trade name Onbrez Breezhaler on November 30, 2009, and by the United States Food and Drug Administration (FDA), under the trade name Arcapta Neohaler, on July 1, 2011. It needs to be taken only once a day, unlike the related drugs formoterol and salmeterol. It is licensed only for the treatment of chronic obstructive pulmonary disease (COPD) (long-term data in patients with asthma are thus far lacking). It is delivered as an aerosol formulation through a dry powder inhaler.
Status:
US Previously Marketed
Source:
DORIBAX by SHIONOGI INC
(2007)
Source URL:
First approved in 2007
Source:
DORIBAX by SHIONOGI INC
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Doripenem is a synthetic carbapenem that has broad antibacterial potency against aerobic and anaerobic gram-positive and gram-negative bacteria. Doripenem is structurally related to beta-lactam antibiotics and shares the bactericidal mode of action of other β-lactam antibiotics by targeting penicillin-binding proteins (PBPs) to inhibit the biosynthesis of the bacterial cell wall. Doripenem is resistant to hydrolysis by most β-lactamases and is resistant to inactivation by renal dehydropeptidases. Doripenem has many similarities to the other carbapenems, as well as some important differences, such as greater potency against Pseudomonas aeruginosa. It was found to be similar to comparator agents. The most common adverse effects related to doripenem therapy were headache, nausea, diarrhea, rash, and phlebitis.
Status:
US Previously Marketed
Source:
FACTIVE by LG CHEM LTD
(2003)
Source URL:
First approved in 2003
Source:
FACTIVE by LG CHEM LTD
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin mesylate is marketed under the brand name Factive, indicated for the treatment of bacterial infection caused by susceptible strains such as S. pneumoniae, H. influenzae, H. parainfluenzae, or M. catarrhalis, S. pneumoniae (including multi-drug resistant strains [MDRSP]), M. pneumoniae, C. pneumoniae, or K. pneumoniae. Gemifloxacin has in vitro activity against a wide range of Gram-negative and Grampositive
microorganisms. Gemifloxacin is bactericidal with minimum bactericidal concentrations (MBCs) generally within one dilution of the minimum inhibitory
concentrations (MICs). Gemifloxacin acts by inhibiting DNA synthesis through the
inhibition of both DNA gyrase and topoisomerase IV (TOPO IV), which are essential for
bacterial growth. Streptococcus pneumoniae showing mutations in both DNA gyrase and
TOPO IV (double mutants) are resistant to most fluoroquinolones. Gemifloxacin has the
ability to inhibit both enzyme systems at therapeutically relevant drug levels in S.
pneumoniae (dual targeting), and has MIC values that are still in the susceptible range for
some of these double mutants.
Status:
US Previously Marketed
Source:
POVAN by PARKE DAVIS
(1959)
Source URL:
First approved in 1955
Class (Stereo):
CHEMICAL (ACHIRAL)
Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Pyrvinium has being shown to be a potent inhibitor of Wnt signaling (EC(50) of ∼10 nM). Pyrvinium binds all casein kinase 1 (CK1) family members in vitro at low nanomolar concentrations and pyrvinium selectively potentiates casein kinase 1α (CK1α) kinase activity. Pyrvinium pamoate (PP) is a potent noncompetitive inhibitor of the androgen receptor (AR). A noncompetitive AR inhibitor pyrvinium has significant potential to treat CRPC, including cancers driven by ligand-independent AR signaling.
Status:
US Previously Marketed
Source:
METATENSIN #2 by SANOFI AVENTIS US
(1982)
Source URL:
First approved in 1954
Source:
SERPASIL by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.
Status:
Possibly Marketed Outside US
First approved in 2014
Source:
Ocuvel by Adler-Stern Pharmaceuticals, LLC
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Zeaxanthin is one of the most common carotenoid alcohols found in nature. It is synthesized in plants and some micro-organisms. Lutein and Zeaxanthin are found in the macula of the human retina, as well as the human crystalline lens. They play a role in protection against age-related macular degeneration (ARMD) and cataract formation. The antioxidant properties of lutein and zeaxanthin together with ocular antioxidants (selenium, zinc, copper, vitamin A, C, E, etc.) inhibit free radical damage caused by light and oxygen. Zeaxanthin supplements are typically taken on the supposition of supporting eye health. It is is Generally Recognized As Safe by FDA.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Elobixibat is the first in class ileal bile acid transporter (IBAT) inhibitor. IBAT inhibitors block ileal absorption of bile acids by: (1) interrupting the enterohepatic circulation of bile resulting in a fall in serum cholesterol and (2) increasing the delivery of bile acids into the colon. Elobixibat stimulates both motor and secretory functions in the colon. Elobixibat is approved in Japan for the treatment of chronic constipation. Elobixibat has potential benefit in the treatment of non-alcoholic steatohepatitis.
Status:
Possibly Marketed Outside US
Source:
NCT03249337: Phase 4 Interventional Recruiting Fuchs' Endothelial Dystrophy
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Ripasudil (K-115) is a selective Rho-associated coiled coil-containing protein kinase (ROCK) inhibitor. This compound, which was originally discovered by D. Western Therapeutics Institute, Inc., reduces intraocular pressure (IOP) by directly acting on the trabecular meshwork, thereby increasing conventional outflow through the Schlemm's canal. As a result of this mechanism of action, ripasudil may offer additive effects in the treatment of glaucoma and ocular hypertension when used in combination with agents such as prostaglandin analogues (which increase uveoscleral outflow) and β blockers (which reduce aqueous production). GLANATEC® (Ripasudil hydrochloride hydrate) ophthalmic solution 0.4% is launched in Japan for the treatment of glaucoma and ocular hypertension.