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Showing 1 - 6 of 6 results
Status:
US Approved Rx
(2020)
Source:
NDA212801
(2020)
Source URL:
First approved in 2020
Source:
NDA212801
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Osilodrostat (INN, USAN) (developmental code name LCI-699) is an orally active, non-steroidal corticosteroid biosynthesis inhibitor which is under development by Novartis for the treatment of Cushing's syndrome and pituitary ACTH hypersecretion (a specific subtype of Cushing's syndrome). Osilodrostat specifically acts as a potent and selective inhibitor of aldosterone synthase (CYP11B2) and at higher dosages of 11β-hydroxylase (CYP11B1). Osilodrostat decreases plasma and urinary aldosterone levels and rapidly corrects hypokalemia, in patients with primary aldosteronism and hypertension. At doses ≥1 mg o.d. Osilodrostat markedly increases 11-deoxycortisol plasma levels and blunts ACTH-stimulated cortisol release in ≈20% of patients, consistent with the inhibition of CYP11B1. In patients with resistant hypertension, Osilodrostat produces a non-significant reduction in blood pressure, possibly due to the increase in 11-deoxycortisol levels and the stimulation of the hypothalamic-pituitary-adrenal feedback axis. Because of the lack of selectivity, poor antihypertensive effect, and short half-life, the development of Osilodrostat as antihypertensive was halted. As of 2017, Osilodrostat is in phase III and phase II clinical trials for the treatment of pituitary ACTH hypersecretion and Cushing's syndrome, respectively.
Status:
US Approved Rx
(2003)
Source:
ANDA076226
(2003)
Source URL:
First approved in 1993
Source:
DEMADEX by ROCHE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Torasemide is a pyridine-sulfonylurea type loop diuretic mainly used for the treatment of edema associated with congestive heart failure, renal disease, or hepatic disease. Also for the treatment of hypertension alone or in combination with other antihypertensive agents. It is also used at low doses for the management of hypertension. It is marketed under the brand name Demadex. Torasemide inhibits the Na+/K+/2Cl--carrier system (via interference of the chloride binding site) in the lumen of the thick ascending portion of the loop of Henle, resulting in a decrease in reabsorption of sodium and chloride. This results in an increase in the rate of delivery of tubular fluid and electrolytes to the distal sites of hydrogen and potassium ion secretion, while plasma volume contraction increases aldosterone production. The increased delivery and high aldosterone levels promote sodium reabsorption at the distal tubules, and by increasing the delivery of sodium to the distal renal tubule, torasemide indirectly increases potassium excretion via the sodium-potassium exchange mechanism. Torasemide's effects in other segments of the nephron have not been demonstrated. Thus torasemide increases the urinary excretion of sodium, chloride, and water, but it does not significantly alter glomerular filtration rate, renal plasma flow, or acid-base balance. Torasemide's effects as a antihypertensive are due to its diuretic actions. By reducing extracellular and plasma fluid volume, blood pressure is reduced temporarily, and cardiac output also decreases.
Status:
Possibly Marketed Outside US
Source:
MIF900002
(2009)
Source URL:
First approved in 2009
Source:
MIF900002
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Metomidate is a non-barbiturate imidazole which produces a sleepy condition of 20-60 minutes duration without substantial analgesia. Since the beginning of 1997 the use of the hypnotic drug metomidate (Hypnodil) in swine is nor longer allowed. This ban caused a substantial therapeutic deficit for anesthesia in swine. 11C-metomidate may be used with positron emission tomography which can differentiate adrenocortical from nonadrenocortical tumors and a suspected adrenocortical cancer may be characterized and staged before surgery. Metomidate hydrochloride is for the sedation and anesthesia of aquarium and non-food fish species. Aquacalm has been granted Indexed status by the FDA for this purpose.
Status:
US Approved Rx
(2020)
Source:
NDA212801
(2020)
Source URL:
First approved in 2020
Source:
NDA212801
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Osilodrostat (INN, USAN) (developmental code name LCI-699) is an orally active, non-steroidal corticosteroid biosynthesis inhibitor which is under development by Novartis for the treatment of Cushing's syndrome and pituitary ACTH hypersecretion (a specific subtype of Cushing's syndrome). Osilodrostat specifically acts as a potent and selective inhibitor of aldosterone synthase (CYP11B2) and at higher dosages of 11β-hydroxylase (CYP11B1). Osilodrostat decreases plasma and urinary aldosterone levels and rapidly corrects hypokalemia, in patients with primary aldosteronism and hypertension. At doses ≥1 mg o.d. Osilodrostat markedly increases 11-deoxycortisol plasma levels and blunts ACTH-stimulated cortisol release in ≈20% of patients, consistent with the inhibition of CYP11B1. In patients with resistant hypertension, Osilodrostat produces a non-significant reduction in blood pressure, possibly due to the increase in 11-deoxycortisol levels and the stimulation of the hypothalamic-pituitary-adrenal feedback axis. Because of the lack of selectivity, poor antihypertensive effect, and short half-life, the development of Osilodrostat as antihypertensive was halted. As of 2017, Osilodrostat is in phase III and phase II clinical trials for the treatment of pituitary ACTH hypersecretion and Cushing's syndrome, respectively.
Status:
US Approved Rx
(2003)
Source:
ANDA076226
(2003)
Source URL:
First approved in 1993
Source:
DEMADEX by ROCHE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Torasemide is a pyridine-sulfonylurea type loop diuretic mainly used for the treatment of edema associated with congestive heart failure, renal disease, or hepatic disease. Also for the treatment of hypertension alone or in combination with other antihypertensive agents. It is also used at low doses for the management of hypertension. It is marketed under the brand name Demadex. Torasemide inhibits the Na+/K+/2Cl--carrier system (via interference of the chloride binding site) in the lumen of the thick ascending portion of the loop of Henle, resulting in a decrease in reabsorption of sodium and chloride. This results in an increase in the rate of delivery of tubular fluid and electrolytes to the distal sites of hydrogen and potassium ion secretion, while plasma volume contraction increases aldosterone production. The increased delivery and high aldosterone levels promote sodium reabsorption at the distal tubules, and by increasing the delivery of sodium to the distal renal tubule, torasemide indirectly increases potassium excretion via the sodium-potassium exchange mechanism. Torasemide's effects in other segments of the nephron have not been demonstrated. Thus torasemide increases the urinary excretion of sodium, chloride, and water, but it does not significantly alter glomerular filtration rate, renal plasma flow, or acid-base balance. Torasemide's effects as a antihypertensive are due to its diuretic actions. By reducing extracellular and plasma fluid volume, blood pressure is reduced temporarily, and cardiac output also decreases.
Status:
Possibly Marketed Outside US
Source:
MIF900002
(2009)
Source URL:
First approved in 2009
Source:
MIF900002
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Metomidate is a non-barbiturate imidazole which produces a sleepy condition of 20-60 minutes duration without substantial analgesia. Since the beginning of 1997 the use of the hypnotic drug metomidate (Hypnodil) in swine is nor longer allowed. This ban caused a substantial therapeutic deficit for anesthesia in swine. 11C-metomidate may be used with positron emission tomography which can differentiate adrenocortical from nonadrenocortical tumors and a suspected adrenocortical cancer may be characterized and staged before surgery. Metomidate hydrochloride is for the sedation and anesthesia of aquarium and non-food fish species. Aquacalm has been granted Indexed status by the FDA for this purpose.