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Status:
US Approved Rx
(2025)
Source:
NDA217906
(2025)
Source URL:
First approved in 2014
Source:
NDA206494
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Avibactam (formerly NXL104, AVE1330A) is a synthetic non-β-lactam, covalent, slowly reversible β-lactamase inhibitor that inhibits the activities of Ambler class A and C β-lactamases and some Ambler class D enzymes. The combination of ceftazidime with avibactam exhibited broad-spectrum activity against Ambler class A- and class C-producing Enterobacteriaceae. AVYCAZ is a combination of ceftazidime, a cephalosporin, and avibactam indicated for the treatment of patients with the following infections caused by designated susceptible microorganisms: Complicated Intra-abdominal Infections, used in combination with metronidazole and Complicated Urinary Tract Infections, including Pyelonephritis.
Status:
US Approved Rx
(1998)
Source:
ANDA075028
(1998)
Source URL:
First approved in 1984
Source:
TRENTAL by VALIDUS PHARMS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Pentoxil (Pentoxifylline Extended-release Tablets, USP) is indicated for the treatment of patients with intermittent claudication based on chronic occlusive arterial disease of the limbs. Pentoxil can improve function and symptoms but is not intended to replace more definitive therapy, such as surgical bypass, or removal of arterial obstructions when treating peripheral vascular disease. Pentoxifylline and its metabolites improve the flow properties of blood by decreasing its viscosity. In patients with chronic peripheral arterial disease, this increases blood flow to the affected microcirculation and enhances tissue oxygenation. The precise mode of action of pentoxifylline and the sequence of events leading to clinical improvement are still to be defined. Pentoxifylline inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, pentoxifylline also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity. It is also a non-selective adenosine receptor antagonist. Pentoxifylline administration has been shown to produce dose-related hemorrheologic effects, lowering blood viscosity, and improving erythrocyte flexibility. Pentoxifylline has been shown to increase leukocyte deformability and to inhibit neutrophil adhesion and activation. Tissue oxygen levels have been shown to be significantly increased by therapeutic doses of pentoxifylline in patients with peripheral arterial disease. Clinical trials were conducted using either extended-release pentoxifylline tablets for up to 60 weeks or immediate-release pentoxifylline capsules for up to 24 weeks. Dosage ranges in the tablet studies were 400 mg bid to tid and in the capsule studies, 200-400 mg tid. The incidence of adverse reactions was higher in the capsule studies (where dose related increases were seen in digestive and nervous system side effects) than in the tablet studies. Studies with the capsule include domestic experience, whereas studies with the extended-release tablets were conducted outside the U.S.
Status:
US Approved OTC
Source:
21 CFR 358.310 ingrown toenail sodium sulfide (aqueous)
Source URL:
First approved in 2003
Source:
21 CFR 358D
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
A sulfide ion is composed of a lone sulfur atom. Its charge is negative two, giving sulfides this formula: S^2-. Sulfide is a strong base, so solutions of sulfide in water are basic, due to hydrolysis. One well-known ionic compound with a sulfide ion is H_2S. The infamous rotten-egg smell often associated with sulfur originates from this compound. Sodium sulfide nonahydrate is used in the formation of surface functionalized cadmium sulfide quantum dots.
Status:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Locicortolone is an anti-inflammatory and antiallergic synthetic glucocorticoid. It has high glucocorticoid cytoplasmic receptor binding affinity in vitro (more than four times higher than dexamethasone) but comparable to dexamethasone relative TAT (tyrosine aminotransferase induction) activity. It has six times lower binding affinity to mineralocorticoid receptor in comparison to dexamethasone.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Binospirone (MDL-73,005-EF) acts as a potent, highly selective 5-HT1A ligand: as an antagonist at postsynaptic 5-HT1A receptors and also acts as a highly efficacious partial agonist at somatodendritic autoreceptors. Experiments on rodents have shown, that it also possesses anxiolytic properties.
Class (Stereo):
CHEMICAL (ACHIRAL)
Fananserin is a potential antipsychotic compound with a high affinity for both D4 and 5-HT2A receptors, and negligible affinity for D2 receptors. Fananserin has been researched for the treatment of schizophrenia. Fananserin was the first selective D4/5-HT2A antagonist to undergo clinical trials for schizophrenia. It has a high affinity for D4 (Ki 2.9 nM) and 5-HT2A (Ki 0.37 nM) receptors and is over 100-fold selective versus H1, a1 adrenergic, 5-HT1A and D2 dopamine receptors. Development of this compound was halted following
phase II clinical trials due to lack of efficacy.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
The novel compounds clamikalant (HMR 1883) or its sodium salt HMR 1098) have been shown to block selectively Kir6.2/SUR1-composed K(ATP) channels. Clamikalant is under development by Aventis Pharma (formerly Hoechst Marion Roussel) for the potential treatment of heart arrest and ventricular arrhythmias. Nevertheless, clamikalant and its sodium salt did not pass the clinical trials
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Piclamilast (RP 73401), is a selective PDE4 inhibitor. It is comparable to other PDE4 inhibitors for its anti-inflammatory effects. It has been investigated for its applications to the treatment of conditions such as asthma, dermatitis, rheumatoid arthritis. Emesis is the most commonly cited side effect of piclamilast.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
HMR 1031 is a potent and specific antagonist of the integrin VLA-4 (alpha4beta1) binding to vascular cell adhesion molecule-1 (VCAM-1) and fibronectin. HMR 1031 is an inhaled drug being developed for the treatment of asthma using an Ultrahaler dry-powder inhalation device. The interaction
of VLA-4 with VCAM-1 is involved in the extravasations, activation, and extravascular survival of mononuclear leukocyte and eosinophil cell types at
sites of airway inflammation. Thus, the VLA-4 antagonist, HMR 1031, has potential as an anti-inflammatory agent.
VIGABATRIN, R-(-)- is an inactive enantiomer of gamma-vinyl-gamma-aminobutyric acid. Vigabatrin exists as a 50/50 racemic mixture of two enantiomers. It is an irreversible inhibitor of the GABA-transaminase, the enzyme responsible for the catabolism of GABA, thus increasing the GABAergic transmission. This drug is mainly prescribed for the treatment of West syndrome, a deleterious pediatric epileptic syndrome also known as infantile spasms. The maximum and minimum plasma concentrations of vigabatrin at steady-state were lower for the S(+) than for the R(-) enantiomer, while the apparent oral clearance was higher for the S(+) than for the R(-) enantiomer in a patient affected with tuberous sclerosis who developed major agitation and aggression and in whom impaired renal function was diagnosed. The question remains of the potential toxicity of the high levels of the R(-) enantiomer. The placental uptake of the active S(+)-isomer from the maternal circulation exceeded that of the R(-)-isomer and this was reflected by a corresponding difference in placental tissue concentrations.