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Status:
Possibly Marketed Outside US
Source:
CELIPTIUM by Institut Gustave-Roussy|Sanofi
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Elliptinium is an antineoplastic agent, which was used in the treatment of metastatic breast cancer in France under the name Celiptium. The drug is known to intercalate into DNA and inhibit topoisomerase II. Several studies have demonstrated that this molecule can be oxidized, yielding a reactive electrophilic form, which is able to bind covalently to a nucleophilic biological molecule.
Status:
Possibly Marketed Outside US
Source:
FLUGESTONE ACETATE by Searle
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
FLUROGESTONE (9α-FLUORO-11β,17α-DIHYDROXYPROGESTERONE) is a steroidal progestin of the 17α-hydroxyprogesterone group that was never marketed. An acetate ester, flurogestone acetate, is used in veterinary medicine. It has progestational action
higher than that of progesterone itself. It is intended for intravaginal use in sheep and goats to
induce oestrus synchronisation. The proposed dosage is 1 sponge, impregnated with 30, 40 (for
sheep) or 45 mg (for goats) flugestone acetate, which is to be removed after 12 to 14 days from
ewes and after 17 to 21 days from goats. Flugestone acetate is not indicated for use in humans.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Aclarubicin (INN) or aclacinomycin A is an anthracycline drug is primarily indicated in conditions like Acute non-lymphoblastic leukemia, Breast cancer, Gastric cancer, Lymphoma, Ovarian coma, Small cell lung cancer, Thyroid cancer. Soil bacteria Streptomyces galilaeus can produce aclarubicin. Aclarubicin (HCl) is used in combination with different anticancerous drugs to obtain best therapeutic results and to reduce toxicity or side effects. Aclarubicin (HCl) is administered intravenously. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin.
Status:
Possibly Marketed Outside US
Source:
MUCOSOLVAN by Boehringer Ingelheim
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ambroxol, a substituted benzylamine, is an active
metabolite of bromhexine, which is itself
a synthetic derivative of vasicine, the active principle extracted from the plant species Adhatoda vasica. Ambroxol is an expectorant exerting mucokinetic properties, mucociliary activity, stimulation of surfactant production, anti-inflammatory and antioxidative actions and the local anaesthetic effect. Ambroxol was discovered at and has been manufactured by Dr. Karl Thomae GmbH, a division of Boehringer Ingelheim. The ambroxol patent is expired and the drug is available as a generic product from many different companies. Ambroxol was originally developed by Boehringer Ingelheim as a OTC therapy for respiratory disorders related to excessive mucus. Ambroxol's indication is secretolytic therapy in acute and chronic bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport. Boehringer Ingelheim markets the product under various brand names such as Mucosolvan® and Lasolvan®. Ambroxol was identified and found to be a pH-dependent, mixed-type inhibitor of glucocerebrosidase (GCase). Its inhibitory activity was maximal at neutral pH, found in the endoplasmic reticulum, and undetectable at the acidic pH of lysosomes. The pH dependence of Ambroxol to bind and stabilize the enzyme was confirmed. Ambroxol increases both the lysosomal fraction and the enzymatic activity of several mutant GCase variants. This profile of Ambroxol would allow to bind and stabilize GCase in the endoplasmic reticulum (thus preventing its degradation within endoplasmic reticulum), but without affecting GCase in the lysosomes (thus allowing it to degrade glucosylceramide). Indeed, studies showed that Ambroxol treatment significantly increased N370S and F213I mutant GCase activity and protein levels in fibroblasts originally obtained from Gaucher patients. Gaucher's disease is caused by the deficiency of glucocerebrosidase; ambroxol is a chaperone that acts by binding to and stabilising glucocerebrosidase. Zywie (formerly ExSAR Corporation) and Belrose Pharma are developing ambroxol hydrochloride (BEL 0218) for the treatment of type III Gaucher's disease.
.
Status:
Possibly Marketed Outside US
Source:
NCT01892488: Phase 4 Interventional Completed Chronic Obstructive Pulmonary Disease (COPD)
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
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
Source:
Miretilan by Sandoz [W. Germany]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Endralazine (6-benzoyl-3-hydrazino-5,6,7,8-tetrahydropyrido-(4,3-c)-pyridazine mesylate) is a peripheral vasodilator drug, which acts by direct relaxation of the smooth muscle fibres of the peripheral arterial vessels. Endralazine has been used as an antihypertensive agent.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Iobenguane, mainly use as a radiopharmaceutical, used in a scintigraphy method called MIBG scan. Synthetic guanethidine derivative that locates phaeochromocytomas and neuroblastomas. The radioisotope used can either be iodine-123 for imaging or iodine-131 for destruction of tissues that metabolize noradrenaline. Iodine 123 is a cyclotron-produced radionuclide that decays to Te 123 by electron capture. Images are produced by a I123 MIBG scintigraphy. It localizes to adrenergic tissue and thus can be used to identify the location of tumors such as pheochromocytomas and neuroblastomas. With I-131 it can also be used to eradicate tumor cells that take up and metabolize norepinephrine. The radioactive iodine component is responsible for its imaging properties. Iobenguane and guanethidine are substrates for the norepinephrine transporter (NET) and accumulate by the uptake mechanism into presynaptic nerve endings. Unlike norepinephrine, these drugs are protonated under physiologic conditions; therefore, they do not cross the blood–brain barrier and in vivo uptake is limited primarily to systemic neuronal tissue. The accumulation of iobenguane in myocardial tissue is also dictated by the high fraction of aortic blood flow that enters the coronary arteries. This physiology constitutes an ideal molecular targeting mechanism for diagnosis of various cardiac diseases, including heart failure, heart transplant rejection, ischemic heart disease, dysautonomia, and drug-induced cardiotoxicity, as well as cardiac neuropathy related to diabetes mellitus and Parkinson disease
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Bunamidine is a anti-parasitic drug, which was approved by FDA for the treatment of tapeworms in cats and dogs (Scolaban 400 tablets).
Status:
Possibly Marketed Outside US
Source:
Adimolol hydrochloride
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Adimolol is an antihypertensive agent with a potent antagonist of central beta-adrenoceptors and has a weaker alpha 1-adrenolytic action. The central alpha 2-antagonistic effect is either very weak or absent. The reduction in beta-adrenoceptor number following adimolol suggests that this prolonged effect may not be solely due to competitive antagonism but may additionally depend upon non-competitive antagonism at beta-adrenoceptors. Adimolol reduced supine, standing and exercise heart rates in a dose dependent manner.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Thiazinamium is an anti-cholinergic phenothiazine deriva¬tive, which also has antihistaminic properties. Intramuscular injection of Thiazinamium induces considerable bronchodilatation, but inconsistent results have been obtained after oral administration. The bioavailability of oral Thiazinamium is only 2-3% of that occurring after intramuscular injection. Intrarectal Thiazinamium is slightly better absorbed (3-9%). The elimination half-life of the parenteral drug is short, being about 20 minutes in most patients. Thiazinamium has been available for the treatment of asthma since the early 1960s but currently withdrawn in most countries. Compared with inhaled ipratropium bromide, intramuscular Thiazinamium and intramuscular atropine were associated with 'extremely frequent side-effects’. Notable tachycardia occurred shortly after intramuscular injection of Thiazinamium in two trials. Dry mouth was reported as ‘frequent’ with oral Thiazinamium, and micturition problems of moderate severity affected 13% of patients.