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Daclatasvir
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DB09102 |
[Daclatasvir is a direct-acting antiviral agent against Hepatitis C Virus (HCV) used for the treatment of chronic HCV genotype 1 and 3 infection. It is marketed under the name DAKLINZA and is contained in daily oral tablets as the hydrochloride salt form . Hepatitis C is an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients [L852]. Daclatasvir was the first drug with demonstrated safety and therapeutic efficacy in treating HCV genotype 3 without the need for co-administration of interferon or [DB00811]. It exerts its antiviral action by preventing RNA replication and virion assembly via binding to NS5A, a nonstructural phosphoprotein encoded by HCV. Binding to the N-terminus of the D1 domain of NS5A prevents its interaction with host cell proteins and membranes required for virion replication complex assembly. Daclatasvir is shown to target both the cis- and trans-acting functions of NS5A and disrupts the function of new HCV replication complexes by modulating the NS5A phosphorylation status [A19640]. The most common critical NS5A amino acid substitutions that led to reduced susceptibility to daclatasvir therapy occured at position Q30 (Q30H/K/R) and M28 in genotype 1a patients and Y93H in genotype 3 patients.
According to 2017 American Association for the Study of Liver Diseases (AASLD), 60mg of daclatasvir is recommended with 400mg [DB08934] for genotype 1a/b patients with or without cirrhosis as second-line therapy. The same dosing regimen can be used as first-line therapy in patients with genotype 3 without cirrhosis and second-line therapy in genotype 3 patients with compensated cirrhosis. Combination therapies that include daclatasir can be used for challenging-to-treat patients who have HIV-1 coinfection, advanced cirrhosis, or post-liver transplant recurrence of HCV [L863]. The therapy is intended to cure or achieve a sustained virologic response (SVR12), after 12 weeks of daily therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality [A19626].
Daclatasvir was FDA-approved in July 2015 for use with [DB08934] (Sovaldi) with or without [DB00811] to treat HCV genotype 1 and 3 infections. The SVR12 in HCV genotype 1a-infected treatment-naïve subjects without and with cirrhosis undergoing daclatasvir and [DB08934] therapy were 88% and 99%, respectively [FDA Label]. The same dosing regimen in treatment-naïve patients with HCV genotype 3 infection with or without cirrhosis achieved SVR12 rates of 71% and 98%, respectively [FDA Label].] |
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Clidinium
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DB00771 |
[Clidinium is a synthetic anticholinergic agent which has been shown in experimental and clinical studies to have a pronounced antispasmodic and antisecretory effect on the gastrointestinal tract. It inhibits muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites. It is used for the treatment of peptic ulcer disease and also to help relieve abdominal or stomach spasms or cramps due to colicky abdominal pain, diverticulitis, and irritable bowel syndrome.] |
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Asfotase alfa
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DB09105 |
[Asfotase alfa is a first-in-class bone-targeted enzyme replacement therapy designed to address the underlying cause of hypophosphatasia (HPP)—deficient alkaline phosphatase (ALP). Hypophosphatasia is almost always fatal when severe skeletal disease is obvious at birth. By replacing deficient ALP, treatment with Asfotase Alfa aims to improve the elevated enzyme substrate levels and improve the body's ability to mineralize bone, thereby preventing serious skeletal and systemic patient morbidity and premature death. Asfotase alfa was first approved by Pharmaceuticals and Medicals Devices Agency of Japan (PMDA) on July 3, 2015, then approved by the European Medicine Agency (EMA) on August 28, 2015, and was approved by the U.S. Food and Drug Administration (FDA) on October 23, 2015. Asfotase Alfa is marketed under the brand name Strensiq® by Alexion Pharmaceuticals, Inc. The annual average price of Asfotase Alfa treatment is $285,000.] |
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Alprostadil
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DB00770 |
[Alprostadil is produced endogenously and causes vasodilation by means of a direct effect on vascular and ductus arteriosus (DA) smooth muscle, preventing or reversing the functional closure of the DA that occurs shortly after birth. This results in increased pulmonary or systemic blood flow in infants. In infants, it is used for palliative, not definitive, therapy to temporarily maintain the patency of the ductus arteriosus until corrective or palliative surgery can be performed in neonates who have congenital heart defects and who depend upon the patent ductus for survival. In adults, it is used for the treatment of erectile dysfunction due to neurogenic, vasculogenic, psychogenic, or mixed etiology.] |
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Magnesium hydroxide
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DB09104 |
[Magnesium hydroxide is an inorganic compound. It is naturally found as the mineral brucite. Magnesium hydroxide can be used as an antacid or a laxative in either an oral liquid suspension or chewable tablet form.
Additionally, magnesium hydroxide has smoke suppressing and flame retardant properties and is thus used commercially as a fire retardant.
It can also be used topically as a deodorant or for the relief of canker sores (aphthous ulcers).] |
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Stiripentol
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DB09118 |
[Stiripentol is an anticonvulsant drug used in the treatment of epilepsy as an adjunct therapy along with [DB00349] and [DB00313]. This drug is currently approved in the USA, Canada, and European countries as oral tablets marketed as Diacomit. FDA approval of this drug was granted on August 20, 2018 [L4352], [F1240]. Unrelated to other anticonvulsants, stiripentol belongs to the group of aromatic allylic alcohols and may potentiate the effect of other antiepileptic drugs (AEDs) due to pharmacokinetic interactions. It elevates the levels of gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter that regulates electrical activity in the central nervous system.] |
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Nitenpyram
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DB11438 |
[Nitenpyram is an insecticide used in agriculture and veterinary medicine to kill external parasites of pets. It is a neonicotinoid, a neurotoxin that blocks neural messages and binds particularly tightly in the central nervous system of insects, causing rapid death.] |
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Nitarsone
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DB11437 |
[Nitarsone is an organoarsenic compound. It is used as an additive in poultry feed to improve weight gain and feed efficiency, while preventing blackhead disease. It is marketed as Histostat by Zoetis, a publicly traded subsidiary of Pfizer.] |
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Paraldehyde
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DB09117 |
[Paraldehyde was initially introduced into medical practice in the United Kingdom in 1882 by the Italian physician Vincenzo Cervello. It is classified as a central nervous system (CNS) depressant and has also been found to be an effective anticonvulsant, hypnotic and sedative agent due to its CNS depressant properties. Paraldehyde is used as an ingredient in some cough medicines as an expectorant, but its efficacy for this indication has not been confirmed and its use as an expectorant may possibly be due to a placebo effect.] |
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Nifurpirinol
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DB11436 |
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Eslicarbazepine acetate
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DB09119 |
[Eslicarbazepine acetate (ESL) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy. Eslicarbazepine acetate is a prodrug that is rapidly converted to eslicarbazepine, the primary active metabolite in the body. Eslicarbazepine's mechanism of action is not well understood, but it is known that it does exert anticonvulsant activity by inhibiting repeated neuronal firing and stabilizing the inactivated state of voltage-gated sodium channels, thus preventing their return to the activated state during which seizure activity can occur.
Eslicarbazepine acetate is marketed as Aptiom in North America and Zebinix or Exalief in Europe. It is available in 200, 400, 600, or 800mg tablets that are taken once daily, with or without food. Eslicarbazepine acetate is associated with numerous side effects including dizziness, drowsiness, nausea, vomiting, diarrhea, headache, aphasia, lack of concentration, psychomotor retardation, speech disturbances, ataxia, depression and hyponatremia. It is recommended that patients taking eslicarbazepine acetate be monitored for suicidality.] |
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Cicletanine
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DB12766 |
[Cicletanine is under investigation for the treatment of Diabetes, Hypokalemia, Hyponatremia, and Arterial Hypertension.] |
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Gaxilose
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DB12767 |
[Gaxilose has been used in trials studying the diagnostic of Lactose Intolerance.] |
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BCG vaccine
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DB12768 |
[BCG vaccine has been investigated for the treatment of Neoplasms, Bladder Cancer, Neoplasms by Site, Urologic Diseases, and Urologic Neoplasms, among others.] |
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Lometrexol
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DB12769 |
[Lometrexol has been used in trials studying the treatment of Lung Cancer, Drug/Agent Toxicity by Tissue/Organ, and Unspecified Adult Solid Tumor, Protocol Specific.] |
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Rabacfosadine
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DB12762 |
[Rabacfosadine has been used in trials studying the treatment of Multiple Myeloma, Non-Hodgkin's Lymphoma, and Chronic Lymphocytic Leukemia.] |
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Monensin
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DB11430 |
[Monensin is a polyether isolated from _Streptomyces cinnamonensis_ that presents antibiotic properties. It is widely used in ruminant animal feeds.] |
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MK-1496
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DB12763 |
[MK-1496 has been used in trials studying the treatment of Neoplasms and Malignant.] |
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ABC-294640
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DB12764 |
[ABC294640 has been used in trials studying the treatment of Diffuse Large B Cell Lymphoma.] |
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Methyl isocyanate
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DB12765 |
[Methyl isocyanate has been investigated for the treatment of Nosocomial Pneumonia.] |
