Inxight Drugs

Showing 1 - 10 of 13 results

Status:

US Approved Rx (2020)

First approved in 2020

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

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 sp...

PASIREOTIDE

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98H1T17066

Status:

US Approved Rx (2012)

First approved in 2012

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, indicated for the treatment of adult patients with Cushing’s disease for whom pituitary surgery is not a...

KETOCONAZOLE

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R9400W927I

Status:

US Approved Rx (2021)

First approved in 1981

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Conditions:

Ketoconazole is an azole antifungal. Ketoconazole was the first broad-spectrum oral antifungal agent available to treat systemic and superficial mycoses. Evidence of hepatotoxicity associated with its use emerged within the first few years of its app...

SELICICLIB

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0ES1C2KQ94

Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Seliciclib (CYC202, R-roscovitine) is a second-generation orally available cyclin-dependent kinases (CDKs) inhibitor that competes for ATP binding sites on these kinases. It is a direct inhibitor of cyclin CDK2/E, CDK2/A and it has inhibitory effects...

RITANSERIN

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145TFV465S

Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research. In humans, ritanserin increases deep slow-wave sleep, improved liveliness in a variety of psychiatric d...

HX-630

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N564S742U1

Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

HX630 is a synthetic RXR pan-agonist. HX-630 has bein shown to exert anti-proliferative and pro-apoptotic effects in murine pituitary corticotroph tumor AtT20 cells, making HX-630 a new therapeutic candidate for Cushing’s disease. It might also serve...

TRILOSTANE

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L0FPV48Q5R

Status:

US Previously Marketed

First approved in 1984

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Trilostane is a synthetic steroid, which interferes with the formation of both cortisol and aldosterone. It is an inhibitor of 3 beta-hydroxysteroid dehydrogenase. This drug under trade name MODRASTANE was withdrawn from human use in the United Stat...

AMINOGLUTETHIMIDE

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0O54ZQ14I9

Status:

US Previously Marketed

First approved in 1960

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Conditions:

Aminoglutethimide, marketing as Cytadren has been used in the treatment of advanced breast and prostate cancer. It was formerly used for its weak anticonvulsant properties. Cytadren is indicated for the suppression of adrenal function in selected pat...

ients with Cushing’s syndrome. Morning levels of plasma cortisol in patients with adrenal carcinoma and ectopic ACTH producing tumors were reduced on the average to about one half of the pretreatment levels, and in patients with adrenal hyperplasia to about two thirds of the pretreatment levels, during 1-3 months of therapy with Cytadren. Data available from the few patients with adrenal adenoma suggest similar reductions in plasma cortisol levels. Measurements of plasma cortisol showed reductions to at least 50% of baseline or to normal levels in one third or more of the patients studied, depending on diagnostic groups and time of measurement. Because Cytadren does not affect the underlying disease process, it is used primarily as an interim measure until more definitive therapy such as surgery can be undertaken or in cases where such therapy is not appropriate. Only small numbers of patients have been treated for longer than 3 months. A decreased effect or “escape phenomenon” seems to occur more frequently in patients with pituitary dependent Cushing’s syndrome, probably because of increasing ACTH levels in response to decreasing glucocorticoid levels. Cytadren blocks several other steps in steroid synthesis, including the C-11, C-18, and C-21 hydroxylations and the hydroxylations required for the aromatization of androgens to estrogens, mediated through the binding of Cytadren to cytochrome P-450 complexes. A decrease in adrenal secretion of cortisol is followed by an increased secretion of pituitary adrenocorticotropic hormone (ACTH), which will overcome the blockade of adrenocortical steroid synthesis by Cytadren. The compensatory increase in ACTH secretion can be suppressed by the simultaneous administration of hydrocortisone. Since Cytadren increases the rate of metabolism of dexamethasone but not that of hydrocortisone, the latter is preferred as the adrenal glucocorticoid replacement. Although Cytadren inhibits the synthesis of thyroxine by the thyroid gland, the compensatory increase in thyroid-stimulating hormone (TSH) is frequently of sufficient magnitude to overcome the inhibition of thyroid synthesis due to Cytadren. In spite of an increase in TSH, Cytadren has not been associated with increased prolactin secretion. At low doses, aminogluthethimide is only an effective inhibitor of aromatase (Cytochrome P450 11A1), but at higher doses, it effectively blocks Cytochrome P450 11A1 (P450scc) as well. Citadel was marketed previously as an anticonvulsant but was withdrawn from marketing for that indication in 1966 because of the effects on the adrenal gland.