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Oxamniquine
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DB01096 |
[An anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. (From Martidale, The Extra Pharmacopoeia, 31st ed, p121)] |
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Butenafine
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DB01091 |
[Butenafine hydrochloride is a synthetic benzylamine antifungal agent. Butenafine's mechanism of action is believed to involve the synthesis inhibition of sterols. In particular, butenafine acts to inhibit the activity of the squalene epoxidase enzyme that is essential in the formation of sterols necessary for fungal cell membranes.] |
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Pentolinium
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DB01090 |
[Pentolinium is a nicotinic antagonist that has been used as a ganglionic blocking agent in hypertension.] |
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Dimethyl sulfoxide
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DB01093 |
[A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during cryopreservation. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.] |
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Ouabain
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DB01092 |
[A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like digitalis. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-exchanging ATPase.] |
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LCB01-0371
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DB13077 |
[Lcb01 0371 is under investigation in clinical trial NCT01554995 (A Clinical Study, Randomized, Double-blind, Placebo-controlled, Single Dose Study).] |
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KOSN-1724
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DB13078 |
[KOSN-1724 is under investigation in clinical trial NCT01379287 (Dose-Escalation Safety and Pharmacokinetic Study of Iso-Fludelone in Patients With Advanced Solid Tumors).] |
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Tregalizumab
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DB13073 |
[Tregalizumab has been used in trials studying the treatment of Rheumatoid Arthritis.] |
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Macimorelin
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DB13074 |
[Macimorelin, a novel and orally active ghrelin mimetic that stimulates GH secretion, is used in the diagnosis of adult GH deficiency (AGHD). More specifically, macimorelin is a peptidomimetic growth hormone secretagogue (GHS) that acts as an agonist of GH secretagogue receptor, or ghrelin receptor (GHS-R1a) to dose-dependently increase GH levels [A31481]. Growth hormone secretagogues (GHS) represent a new class of pharmacological agents which have the potential to be used in numerous clinical applications. They include treatment for growth retardation in children and cachexia associated with chronic disease such as AIDS and cancer.
Growth hormone (GH) is classically linked with linear growth during childhood. In deficiency of this hormone, AGHD is commonly associated with increased fat mass (particularly in the abdominal region), decreased lean body mass, osteopenia, dyslipidemia, insulin resistance, and/or glucose intolerance overtime. In addition, individuals with may be susceptible to cardiovascular complications from altered structures and function [A31484]. Risk factors of AGHD include a history of childhood-onset GH deficiency or with hypothalamic/pituitary disease, surgery, or irradiation to these areas, head trauma, or evidence of other pituitary hormone deficiencies [A31481]. While there are various therapies available such as GH replacement therapy, the absence of panhypopituitarism and low serum IGF-I levels with nonspecific clinical symptoms pose challenges to the detection and diagnosis of AGHD. The diagnosis of AGHD requires biochemical confirmation with at least 1 GH stimulation test [A31481]. Macimorelin is clinically useful since it displays good stability and oral bioavailability with comparable affinity to ghrelin receptor as its endogenous ligand. In clinical studies involving healthy subjects, macimorelin stimulated GH release in a dose-dependent manner with good tolerability [A31481].
Macimorelin, developed by Aeterna Zentaris, was approved by the FDA in December 2017 under the market name Macrilen for oral solution.] |
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Menaquinone 7
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DB13075 |
[Menaquinone 7 is under investigation in clinical trial NCT00402974 (The Effect of Vitamin K Supplementation on Osteocalcin Carboxylation in Healthy Children).] |
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Yttrium Y-90
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DB13076 |
[Yttrium 90 has been investigated for the treatment of Colon Cancer and Colorectal Cancer.] |
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Surinabant
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DB13070 |
[Surinabant has been investigated for the treatment of Smoking Cessation.] |
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Creatinolfosfate
|
DB13071 |
[COP is under investigation for the treatment of Rheumatoid Arthritis, Mature B-Cell Lymphoma, and Noninflammatory Degenerative Joint Disease. COP has been investigated for the treatment of Diabetic Retinopathy.] |
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GDC-0349
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DB13072 |
[GDC-0349 has been used in trials studying the treatment of Non-Hodgkin's Lymphoma, Solid Tumor.] |
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Flucytosine
|
DB01099 |
[A fluorinated cytosine analog that is used as an antifungal agent.] |
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Rosuvastatin
|
DB01098 |
[Rosuvastatin, also known as the brand name product Crestor, is a lipid-lowering drug that belongs to the statin class of medications, which are used to lower the risk of cardiovascular disease and manage elevated lipid levels by inhibiting the endogenous production of cholesterol in the liver. More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase,[A181421] which catalyzes the conversion of HMG-CoA to mevalonic acid and is the third step in a sequence of metabolic reactions involved in the production of several compounds involved in lipid metabolism and transport including cholesterol, low-density lipoprotein (LDL) (sometimes referred to as "bad cholesterol"), and very low-density lipoprotein (VLDL). Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD, such as those with Type 2 Diabetes. The clear evidence of the benefit of statin use coupled with very minimal side effects or long term effects has resulted in this class becoming one of the most widely prescribed medications in North America.[A181087, A181406]
Rosuvastatin and other drugs from the statin class of medications including [atorvastatin], [pravastatin], [simvastatin], [fluvastatin], and [lovastatin] are considered first-line options for the treatment of dyslipidemia.[A181087, A181406] This is largely due to the fact that cardiovascular disease (CVD), which includes heart attack, atherosclerosis, angina, peripheral artery disease, and stroke, has become a leading cause of death in high-income countries and a major cause of morbidity around the world.[A181084] Elevated cholesterol levels, and in particular, elevated low-density lipoprotein (LDL) levels, are an important risk factor for the development of CVD.[A181087,A181553] Use of statins to target and reduce LDL levels has been shown in a number of landmark studies to significantly reduce the risk of development of CVD and all-cause mortality.[A181090,A181093,A181096,A181427,A181475,A181538] Statins are considered a cost-effective treatment option for CVD due to their evidence of reducing all-cause mortality including fatal and non-fatal CVD as well as the need for surgical revascularization or angioplasty following a heart attack.[A181087, A181406] Evidence has shown that even for low-risk individuals (with <10% risk of a major vascular event occurring within 5 years) statins cause a 20%-22% relative reduction in major cardiovascular events (heart attack, stroke, coronary revascularization, and coronary death) for every 1 mmol/L reduction in LDL without any significant side effects or risks.[A181397, A181403]
While all statin medications are considered equally effective from a clinical standpoint, rosuvastatin is considered the most potent; doses of 10 to 40mg rosuvastatin per day were found in clinical studies to result in a 45.8% to 54.6% decreases in LDL cholesterol levels, which is about three-fold more potent than [atorvastatin]'s effects on LDL cholesterol.[A181409,A1793] However, the results of the SATURN trial[A181427] concluded that despite this difference in potency, there was no difference in their effect on the progression of coronary atherosclerosis.
Rosuvastatin is also a unique member of the class of statins due to its high hydrophilicity which increases hepatic uptake at the site of action, low bioavailability, and minimal metabolism via the Cytochrome P450 system.[A181523] This last point results in less risk of drug-drug interactions compared to [atorvastatin], [lovastatin], and [simvastatin], which are all extensively metabolized by Cytochrome P450 (CYP) 3A4, an enzyme involved in the metabolism of many commonly used drugs.[A181460] Drugs such as [ciclosporin], [gemfibrozil], and some antiretrovirals are more likely to interact with this statin through antagonism of OATP1B1 organic anion transporter protein 1B1-mediated hepatic uptake of rosuvastatin.[F4649, F4652]] |
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Oxiranpseudoglucose
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DB02394 |
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Oxybutynin
|
DB01062 |
[Overactive bladder (OAB) is a common condition negatively impacting the lives of millions of patients worldwide. Due to its urinary symptoms that include nocturia, urgency, and frequency, this condition causes social embarrassment and a poor quality of life.[A185996,A185999]
Oxybutynin, also marketed as Ditropan XL, is an anticholinergic medication used for the relief of overactive bladder symptoms that has been optimized for high levels of safety and efficacy since initial FDA approval in 1975.[A183782,L8648] This drug relieves undesirable urinary symptoms, increasing the quality of life for patients affected by OAB. It is often used as first-line therapy for OAB.[A185990]] |
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3-Hydroxymethyl-5-Aziridinyl-1methyl-2-[1h-Indole-4,7-Dione]-Propanol
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DB02395 |
|
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Azlocillin
|
DB01061 |
[Azlocillin is a semisynthetic ampicillin-derived acylureido penicillin.] |
