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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:
ZELNORM by ALFASIGMA
(2002)
Source URL:
First approved in 2002
Source:
ZELNORM by ALFASIGMA
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tegaserod (3‐(5‐methoxy‐1H‐indol‐3ylmethylene)‐N‐pentyl‐carbazimidamide), an aminoguanidine indole derivative of serotonin, is a selective partial agonist highly selective for 5‐HT4 receptor with an affinity constant in the nanomolar range. Tegaserod, by acting as an agonist at neuronal 5-HT4 receptors, triggers the release of further neurotransmitters such as calcitonin gene-related peptide from sensory neurons. The activation of 5-HT4 receptors in the gastrointestinal tract stimulates the peristaltic reflex and intestinal secretion, as well as inhibits visceral sensitivity. In vivo studies showed that tegaserod enhanced basal motor activity and normalized impaired motility throughout the gastrointestinal tract. Zelnorm® (tegaserod maleate) is indicated for the short-term treatment of women with irritable bowel
syndrome (IBS) whose primary bowel symptom is constipation. In addition Zelnorm® is indicated for the treatment of patients less than 65 years of age with
chronic idiopathic constipation.
Status:
US Previously Marketed
Source:
SULFINPYRAZONE by PAR PHARM
(1985)
Source URL:
First approved in 1959
Source:
ANTURANE by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Sulfinpyrazone was approved by the U.S. Food and Drug Administration (FDA) on May 13, 1959. It was developed and marketed as Anturane® by Novartis. Sulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4). Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs). Branded and generic forms of sulfinpyrazone have been discontinued in the US.
Status:
US Previously Marketed
Source:
GAMENE by SOLA BARNES HIND
(1976)
Source URL:
First approved in 1951
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Lindane is an isomer of hexachlorocyclohexane that has been used both as an agricultural insecticide and as a pharmaceutical. As a shampoo, lindane is used for treamtment lice infestation. Lindane lotion is used for treatment of scabies. Due to toxicities, associated with lindane, it is used only in patients who cannot tolerate or have failed first-line treatment with safer medication. Lindane exerts its parasiticidal action by being directly absorbed into the parasites and their ova, where it interferes with GABA neurotransmitter function by interacting with the GABAA channel complex at the picrotoxin binding site.
Status:
US Previously Marketed
Source:
Santonin U.S.P.
(1921)
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Santonin, a natural compound, is a sesquiterpene lactone. It is known as an anthelmintic drug which was used in the past (19th - early 20th centuries) mainly to treat different kinds of intestinal worms such as roundworm or ascaris lumbricoides except the tapeworm. It was also indicated for use in retention of urine and nocturnal enuresis from atony, urethral irritation with pain at uterine disorders, retention of urine in fevers, deficient spinal innervation, as evidenced by impaired respiration and tympanitis, vesical tenesmus and strangury, retention of urine from the use of opiates. Santonin was formerly listed in U.S. and British pharmacopoeia but due to the severe side effects and the development of many safer deworming drugsa it is no longer registered as a drug in most countries. Originally isolated from the poisons plant Artemisia maritima, santonin is itself a toxic compound. It is the anhydride of santonic acid, which is a derivative of dimethyl-naphtalene. It dissolves in alkalies with formation of salts of this acid. In acetic acid solution, when exposed to sunlight for about a month, santonin is converted into photosantonic acid. Santonin was found to have significant anti-inflammatory activity on acute inflammatory processes and as shown in vitro can activate pregnane X receptors and constitutive androstane receptors and subsequently increases the expression of drug-metabolizing enzymes.
Status:
US Previously Marketed
First marketed in 1921
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Melatonin (5-methoxy N-acetyltryptamine) is a hormone synthesized and released from the pineal gland at night, which acts on specific high affinity G-protein coupled receptors to regulate various aspects of physiology and behaviour, including circadian and seasonal responses, and some retinal, cardiovascular and immunological functions. Melatonin is also made synthetically and available without a prescription as an over-the-counter (OTC) dietary supplement in the U.S. Melatonin supplementation has many uses, however, it has been widely studied for treatment of jet lag and sleep disorders. Parents may consider using melatonin to help their child who has a trouble falling asleep. A medical professional should always evaluate insomnia or other sleeping disorders in children. Additionally, melatonin has been shown to protect against oxidative stress in various, highly divergent experimental systems. There are many reasons for its remarkable protective potential. In mammals, melatonin binds to a number of receptor subtypes including high-affinity (MT1 and MT2) and low-affinity (MT3, nuclear orphan receptors) binding sites, which are distributed throughout the central nervous system and periphery.
Status:
Possibly Marketed Outside US
Source:
M016
(2024)
Source URL:
First approved in 2024
Source:
M016
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Ginkgolide B belongs to the class of organic compounds known as ginkgolides and bilobalides. These are diterpene lactones with a structure based either on the gingkolide or the bilobalide skeleton. The ginkgolide skeleton is a very rigid structure consisting of hexacyclic C20 trilactone. The cis-fused F/A/D/C ring junction forms an empty semi-ball hole, the D ring contains a cage form tetrahydrofuran ring which occupies the center of the empty hole, and the oxygen atoms of the D,C and F ring and 10-hydroxyl group consist of an analogous crown ether structure. Ginkgolide B is one of the ginkgolides isolated from the leaves of the Ginkgo biloba tree. The Ginkgolide B is the most potent antagonist of platelet activating factor (PAF) and exhibits therapeutic action in a variety of diseases mainly by the PAF receptor. The ginkgolide B possesses a number of beneficial effects such as anti-inflammatory, anti-allergic, antioxidant, and neuroprotective effects. It promotes the proliferation, migration and adhesion of endothelial progenitor cells, and the induction of angiogenesis through vascular endothelial factor (VEGF). Ginkgolide B is considered a valid non-pharmacological (or nutraceutical) approach to the prophylaxis of both migraine with and without aura. Effects of ginkgolide B include reduction of Ca2+-stimulated intracellular events, scavenging of free radicals, modulation of central nervous system glutamatergic transmission and reduction of antiplatelet activating factor (PAF) levels in brain. Ginkgolide B is an active component of EGb, a standardised extract of Ginkgo biloba leaves. Ginkgolide B is one of the major components of EGb-761.
Status:
Possibly Marketed Outside US
Source:
Hepad S5 by YOUNGJIN Korean Medicine Clinic
(2021)
Source URL:
First approved in 2021
Source:
Hepad S5 by YOUNGJIN Korean Medicine Clinic
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Honokiol is a biphenolic natural product isolated from the bark and leaves of Magnolia plant spp. Honokiol possesses anti-carcinogenic, anti-inflammatory, anti-oxidative, anti-angiogenic as well as the inhibitory effect on malignant transformation of papillomas to carcinomas in vitro and in vivo animal models without any appreciable toxicity. Honokiol affects multiple signaling pathways, molecular and cellular targets including nuclear factor-κB (NF-κB), STAT3, epidermal growth factor receptor (EGFR), cell survival signaling, cell cycle, cyclooxygenase and other inflammatory mediators, etc. Honokiol can permeate the blood-brain barrier and the blood-cerebrospinal fluid to increase its bioavailability in neurological tissues. Diverse studies have provided evidence on the neuroprotective effect of honokiol in the central nervous system, due to its potent antioxidant activity, and amelioration of the excitotoxicity mainly related to the blockade of glutamate receptors and reduction in neuroinflammation. Honokiol can attenuate neurotoxicity exerted by abnormally aggregated Abeta in Alzheimer's disease. Honokiol is being developed by Huons as HL tablet for the treatment of alcoholic and non-alcoholic fatty liver.
Status:
Possibly Marketed Outside US
First approved in 2015
Source:
21 CFR 352
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Diethyltoluamide (DEET) is an insect repellent used to keep insects away. This product is effective against mosquitoes, biting flies (gnats, sandflies, deer flies, stable flies, black flies), ticks, harvest mites, and fleas. DEET is absorbed through the skin. DEET has few adverse effects when applied as directed. The most common problem is local skin irritation, including erythema and pruritis, at the site of application.
Status:
Possibly Marketed Outside US
Source:
ECTOMETHRIN by National Research Development Corporation
Source URL:
First approved in 2011
Source:
MIF900011
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Conditions:
Cypermethrin is a synthetic, pyrethroid insecticide that has high insecticidal activity, low avian and mammalian toxicity. Cypermethrin works by quickly affecting the insect’s central nervous system. The major target site of cypermethrin is the sodium channel of the nerve membrane. A sodium channel exposed to cypermethrin can remain open much longer, even up to several seconds. It is used to control many pests including lepidopterous pests of cotton, fruit, and vegetable crops. In veterinary, it is applied topically for the control of ectoparasites such as ticks, fleas, lice and blowflies.