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Status:
Possibly Marketed Outside US
Source:
Dirame by Schering
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Propiram is an orally administered analgesic with partial morphine-like agonist and weak antagonist properties. Analgesic efficacy of propiram, usually 50 or 100mg, appears comparable to that of standard dosages of other oral opioid drugs [i.e. pentazocine, pethidine (meperidine)] in patients with acute pain of moderate to severe intensity arising from various gynaecological and surgical procedures, and may be superior to codeine in gynaecological and postoperative dental pain. Propiram is a non-addictive analgesic for the relief of moderate-to-severe pain. Propiram reached Phase III clinical trials in the United States and Canada, but was discontinued. Propiram is a partial opioid mu receptor agonist.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Masitinib is a new orally administered tyrosine kinase inhibitor that targets mast cells and macrophages, important cells for immunity, through inhibiting a limited number of kinases. Based on its unique mechanism of action, masitinib can be developed in a large number of conditions in oncology, in inflammatory diseases, and in certain diseases of the central nervous system. In oncology due to its immunotherapy effect, masitinib can have an effect on survival, alone or in combination with chemotherapy. Through its activity on mast cells and consequently the inhibition of the activation of the inflammatory process, masitinib can have an effect on the symptoms associated with some inflammatory and central nervous system diseases and the degeneration of these diseases. AB Science is developing masitinib in multiple sclerosis and alzheimer's disease. Masitinib targets kinases, including c-Kit, PDGFR, and Lyn. It is used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Mifamurtide (liposomal muramyl tripeptide phosphatidylethanolamine; trade name Mepact) is an immunomodulator with antitumor effects that appear to be mediated via activation of monocytes and macrophages. After intravenous administration, mifamurtide is selectively phagocytosed by monocytes and macrophages. Cytosolic Mifamurtide specifically interacts with nucleotide-binding oligomerization domain 2 (NOD2) receptor that induces nuclear factor (NF)-kB activation and is implicated in innate immune defense. Activation of monocyte-mediated tumoricidal function was observed following in vivo treatment with mifamurtide in phase I/II clinical trials. Intravenous administration of mifamurtide inhibited tumor growth and increased survival in rodent models of lung and liver metastasis. In a large, randomized, open-label, multicenter, phase III trial, the addition of adjuvant (postoperative) mifamurtide to three- or four-drug combination chemotherapy (doxorubicin, cisplatin, and high-dose methotrexate with, or without, ifosfamide) was associated with a statistically significant improvement in overall survival in patients with newly diagnosed, high-grade, non-metastatic, resectable osteosarcoma. The pattern of outcome was generally similar in a small cohort of patients with metastatic disease who were enrolled in this trial. Mifamurtide is generally well tolerated; adverse events attributed to administration of the drug include chills, fever, headache, nausea, and myalgias. In the EU, mifamurtide is indicated in children, adolescents, and young adults for the treatment of high-grade, resectable, non-metastatic osteosarcoma after macroscopically complete surgical resection; it is administered by intravenous infusion in conjunction with postoperative multiagent chemotherapy. In the US, mifamurtide is currently an investigational agent that holds orphan drug status for the treatment of osteosarcoma.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Tilarginine is L-N-monomethyl arginine (L -NMMA), a non-selective inhibitor of nitric oxide synthase (NOS), which has been studied in the treatment of septic shock and cardiogenic shock complicating myocardial infarction. Despite strong evidence that excessive nitric oxide (NO) production plays a pivotal role in the pathogenesis of septic shock and may contribute to the pathogenesis of cardiogenic shock complicating myocardial infarction, outcome studies in these two disorders have proved disappointing. Tilarginine therapy was associated with an excess mortality, particularly at doses > 5 mg/(kg h), in septic shock, whereas the effects of a lower dose (1 mg/(kg h)) in cardiogenic shock complicating myocardial infarction were neutral. The excess mortality in patients with septic shock was almost certainly the result of unfavorable hemodynamic changes induced by Tilarginine (decreased cardiac output, increased pulmonary vascular resistance and reduced tissue oxygen delivery) whereas the lack of benefit in patients with cardiogenic shock complicating myocardial infarction may have been because the dose of Tilarginine was too low.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Diamminedichlorodihydroxyplatinum IV is the platinum-based antineoplasticis agent. Oxaliplatin is cis, cis, trans- isomer of Diamminedichlorodihydroxyplatinum IV. Oxaliplatin show high stability and therefore can be utilized orally for outpatient care. Although oxoplatin is capable of binding directly to DNA after prolonged incubation, platinum(IV) agents are considered to be largely inert prodrugs that are converted to highly cytotoxic platinum(II) compounds by reducing substances, enzymes, or microenvironmental conditions. Reaction of oxoplatin with 0.1 M hydrogen chloride mimicking gastric acid yields cis-diammine-tetrachlorido-platinum(IV) (DATCP[IV]), which exhibits two-fold increased activity. The oxoplatin metabolite DATCP(IV) constitutes a potent cytotoxic derivative that may be produced by gastric acid or acidic areas prevailing in larger solid tumors, depending on the respective pharmaceutical formulation of oxoplatin.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Radium chloride salt of radioactive element radium. It was first isolated in the early 20th century by Marie Curie and André-Louis Debierne. The most stable isotope is radium-226, it has a half-life of 1600 years and occurs naturally as a product of radioactive decay of uranium. Chloride of radium-223 (half-life 11.4 days) is used in medicine as a radiotherapeutic drug. It was approved for the treatment of male patients with symptoms of advanced prostate cancer with bone metastases. Ra 223 mimics calcium and forms complexes with the bone mineral hydroxyapatite at areas of increased bone turnover. The radioactive alpha particles emitted by radium Ra 223 helps in killing cancer cells in the bone by damaging their DNA. Radium Ra 223 causes minimal damage to the nearby healthy cells.
Status:
Possibly Marketed Outside US
Source:
Ophtorenin by Pharma-Schwarz
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Ophthalmic Bupranolol is used for the management of glaucoma and oral Bupranolol is used for the management of cardiovascular disorders. S-Bupranolol has also being shown to have superior preclinical safety profile and great antinociceptive efficacy and should be considered as a unique b-AR compound to advance future clinical pain studies.
Status:
Possibly Marketed Outside US
Source:
Anexate by Roche
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Mefenorex or (+/-)N-(3-chloropropyl)-1-methyl-2-phenylethylamine is an N-alkylated analogue of amphetamine. The therapeutic efficacy of mefenorex as an adjunctive support in the treatment of obesity for limited periods of time, as well as its ability to be well tolerated, has been amply demonstrated. Mefenorex is considered to be racemic mixture, no available data regarding enantiospecific pharmacological activity of the compound.
Status:
Possibly Marketed Outside US
Source:
Survector by Eutherapie [France]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Amineptine is a selective inhibitor of dopamine reuptake. The drug was developed in France and was marketed for the treatment of depressive disorders under the name Survector among the others. Amineptine was withdrawn from the French market in 1999 because of abuse and drug dependence and because of its hepatic (cholestatic injuries) and cutaneous (acne) adverse effects.