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Tea tree oil
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DB11218 |
[Tea tree oil is an essential oil derived mainly from the Australian native plant _Melaleuca alternifolia_ via steam distillation of the of the leaves and terminal branches [A32439]. It may be referred to as _Melaleuca alternifolia_ oil. It has been a popular ingredient in a variety of household and cosmetic products due to its antiseptic, anti-inflammatory, broad-spectrum antimicrobial and antioxidant properties [A32438]. The dermatological use of tea tree oil has been investigated by various studies, where several studies have suggested the uses of this oil for the treatment of acne vulgaris, seborrheic dermatitis, and chronic gingivitis [A32438]. Terpene hydrocarbons and related alcohols constitute tea tree oil, with [DB12816] being the major antimicrobial component [A32439].] |
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Arbutin
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DB11217 |
[Extracted from the dried leaves of bearberry plant in the genus _Arctostaphylos_ and other plants commonly in the _Ericaceae_ family, arbutin is a beta-D-glucopyranoside of [DB09526]. It is found in foods, over-the-counter drugs, and herbal dietary supplements [F43]. Most commonly, it is an active ingredient in skincare and cosmetic products as a skin-lightening agent for the prevention of melanin formation in various skin conditions that involve cutaneous hyperpigmentation or hyperactive melanocyte function [A27248]. It has also been used as an anti-infective for the urinary system as well as a diuretic [F43]. Arbutin is available in both natural and synthetic forms; it can be synthesized from acetobromglucose and [DB09526] [F43]. Arbutin is a competitive inhibitor of tyrosinase (E.C.1.14.18.1) in melanocytes [A27248], and the inhibition of melanin synthesis at non-toxic concentrations was observed _in vitro_. Arbutin was shown to be less cytotoxic to melanocytes in culture compared to [DB09526] [A32942].] |
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Iniparib
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DB13877 |
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Pibrentasvir
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DB13878 |
[Pibrentasvir is a direct acting antiviral agent and Hepatitis C virus (HCV) NS5A inhibitor that targets the the viral RNA replication and viron assembly. In combination with [DB13879], pibrentastiv is a useful therapy for patients who experienced therapeutic failure from other NS5A inhibitors. In cell cultures, the emergence of amino acid substitutions at known NS5A inhibitor resistance-associated positions in HCV genotype 1a, 2a or 3a replicons led to reduced susceptibility and resistance to pibrentasvir [FDA Label]. These resistance-associated amino acid substitutions included Q30D/deletion, Y93D/H/N or H58D +Y93H in genotype 1a replicons, F28S + M31I or P29S + K30G in genotype 2a replicons, and Y93H in genotype 3a replicons. Individual NS5A amino acid substitutions that reduced susceptibility to pibrentasvir include M28G or Q30D in a genotype 1a replicon and P32-deletion in a genotype 1b replicon [FDA Label].
Pibrentasvir is available as an oral combination therapy with [DB13879] under the brand name Mavyret. This fixed-dose combination therapy was FDA-approved in August 2017 to treat adults with chronic hepatitis C virus (HCV) genotypes 1-6 without cirrhosis (liver disease) or with mild cirrhosis, including patients with moderate to severe kidney disease and those who are on dialysis [L940]. Mavyret is also indicated for HCV genotype 1-infected patients who have been previously treated with regimens either containing an NS5A inhibitor or an NS3/4A protease inhibitor, but not both [L940]. Hepatitis C viral infection often leads to decreased liver function and subsequent liver failure, causing a significantly negative impact on the patients' quality of life. The ultimate goal of the combination treatment is to achieve sustained virologic response (SVR) and cure the patients from the infection. In clinical trials, this combination therapy achieved SVR12 rate, or undetectable Hepatitis C for twelve or more weeks after the end of treatment, of ≥93% across genotypes 1a, 2a, 3a, 4, 5 and 6 [FDA Label].] |
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LY-2886721
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DB12547 |
[LY2886721 has been used in trials studying the basic science of Alzheimer's Disease.] |
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Glecaprevir
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DB13879 |
[Glecaprevir is a direct acting antiviral agent and Hepatitis C virus (HCV) NS3/4A protease inhibitor that targets the the viral RNA replication. In combination with [DB13878], glecaprevir is a useful therapy for patients who experienced therapeutic failure from other NS3/4A protease inhibitors. It demonstrates a high genetic barrier against resistance mutations of the virus. In cell cultures, the emergence of amino acid substitutions at NS3 resistance-associated positions A156 or D/Q168 in HCV genotype 1a, 2a or 3a replicons led to reduced susceptibility to glecaprevir [FDA Label]. The combinations of amino acid substitutions at NS3 position Y65H and D/Q168 also results in greater reductions in glecaprevir susceptibility, and NS3 Q80R in genotype 3a patients also leads to glecaprevir resistance [FDA Label].
Glecaprevir is available as an oral combination therapy with [DB13878] under the brand name Mavyret. This fixed-dose combination therapy was FDA-approved in August 2017 to treat adults with chronic hepatitis C virus (HCV) genotypes 1-6 without cirrhosis (liver disease) or with mild cirrhosis, including patients with moderate to severe kidney disease and those who are on dialysis [L940]. Mavyret is also indicated for HCV genotype 1-infected patients who have been previously treated with regimens either containing an NS5A inhibitor or an NS3/4A protease inhibitor, but not both [L940]. Hepatitis C viral infection often leads to decreased liver function and subsequent liver failure, causing a significantly negative impact on the patients' quality of life. The ultimate goal of the combination treatment is to achieve sustained virologic response (SVR) and cure the patients from the infection. In clinical trials, this combination therapy achieved SVR12 rate, or undetectable Hepatitis C for twelve or more weeks after the end of treatment, of ≥93% across genotypes 1a, 2a, 3a, 4, 5 and 6 [FDA Label].] |
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Sparsentan
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DB12548 |
[Sparsentan has been used in trials studying the treatment of Focal Segmental Glomerulosclerosis. Sparsentan is the first and only dual-acting angiotensin and endothelin receptor antagonist (DARA) in development.] |
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Pyrazoloacridine
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DB12549 |
[Pyrazoloacridine has been used in trials studying the treatment of Lung Cancer, Liver Cancer, Breast Cancer, Melanoma (Skin), and Metastatic Cancer, among others.] |
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Enzacamene
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DB11219 |
[Commonly known as 4-methylbenzylidene-camphor (4-MBC), enzacamene is a camphor derivative and an organic chemical UV-B filter. It is used in cosmetic products such as sunscreen to provide skin protection against UV rays. While its effects on the human reproductive system as an endocrine disruptor are being investigated, its use in over-the-counter and cosmetic products is approved by Health Canada. Its tradenames include Eusolex 6300 (Merck) and Parsol 5000 (DSM).] |
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Fenofibric acid
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DB13873 |
[Fenofibrate is a third generation fibric acid derivative that is predominantly administered as monotherapy to decrease elevated low-density lipoprotein cholesterol, total cholesterol, triglycerides, apolipoprotein B and alternatively to increase high-density lipoprotein cholesterol in patients diagnosed with primary hyperlipidemia or mixed dyslipidemia and to reduce triglycerides in patients with severe hypertriglyceridemia [FDA Label, A32038]. Fenofibrate however is generally extremely lipophilic, largely insoluble in water, and poorly absorbed [A32038]. As the primary active metabolite of fenofibrate however, various hydrophilic salt formulations of fenofibric acid have since been developed, resulting in therapeutic agents that demonstrate far greater solubility, absorption throughout the gastrointestinal tract, bioavailability, and capability to be administered irrespective of patient food intake [FDA Label, A32038].] |
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GSK-356278
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DB12542 |
[Gsk356278 has been used in trials studying the treatment and basic science of Anxiety Disorders, Huntington Disease, Depressive Disorder, Huntingtons Disease, and Depressive Disorder, Major, among others.] |
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Ferrous bisglycinate
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DB11210 |
[Ferrous bisglycinate is a chelate that is used as a source of dietary iron. Forming a ring structure when reacting with glycine, ferrous bisglycinate acts as both a chelate and a nutritionally functional [A27250]. It is found in foods for food enrichment or in supplements for the treatment of iron deficiency or iron deficiency anemia.] |
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Enasidenib
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DB13874 |
[Enasidenib is an orally available treatment for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with specific mutations in the isocitrate dehydrogenase 2 (IDH2) gene, which is a recurrent mutation detected in 12-20% of adult patients with AML [A20344, A20345]. Patients eligible for this treatment are selected by testing the presence of IDH2 mutations in the blood or bone marrow. This small molecule acts as an allosteric inhibitor of mutant IDH2 enzyme to prevent cell growth, and it also has shown to block several other enzymes that play a role in abnormal cell differentiation. First developed by Agios Pharmaceuticals and licensed to Celgene, enasidenib was approved by U.S. Food and Drug Administration on August 1, 2017.] |
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Samidorphan
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DB12543 |
[Samidorphan has been used in trials studying the treatment of Schizophrenia, Alcohol Dependence, and Binge Eating Disorder.] |
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Harmaline
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DB13875 |
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Indobufen
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DB12545 |
[Indobufen has been used in trials studying the supportive care and prevention of Atrial Fibrillation.] |
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Brofaromine
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DB13876 |
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Lecozotan
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DB12540 |
[Lecozotan has been used in trials studying the treatment of Alzheimer Disease.] |
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Albendazole oxide
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DB13871 |
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Lormetazepam
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DB13872 |
[Lormatazepam is an orally available benzodiazepine used in the UK for the treatment of short-term insomnia [L927]. It is marketed by Auden Mckenzie (Pharma Division) in 0.5 and 1 mg tablet formulations.] |