Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H33N3O3S |
| Molecular Weight | 419.581 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCSC1=C(C=CC(=N1)N2CCC[C@@H](CC(O)=O)C2)C(=O)NC3CCCCC3
InChI
InChIKey=NCDZABJPWMBMIQ-INIZCTEOSA-N
InChI=1S/C22H33N3O3S/c1-2-13-29-22-18(21(28)23-17-8-4-3-5-9-17)10-11-19(24-22)25-12-6-7-16(15-25)14-20(26)27/h10-11,16-17H,2-9,12-15H2,1H3,(H,23,28)(H,26,27)/t16-/m0/s1
AZD4017, a 11β-hydroxysteroid dehydrogenase type 1 inhibitor, has been developed by AstraZeneca for the treatment of obesity, raised intraocular pressure (IOP) and type 2 diabetes. Inhibition of 11β-HSD1 is an attractive mechanism for the treatment of obesity and other elements of the metabolic syndrome. However, studies were discontinued due to safety and efficacy reasons. Besides, specific inhibition of 11β-HSD1 can decrease intracranial pressure and consequently treat patients with Idiopathic Intracranial Hypertension (IIH), thus AZD4017 participated in phase II clinical trials to treat this disease. IIH, also known as benign intracranial hypertension or pseudotumor cerebri, is a condition of unknown etiology characterized by elevated intracranial pressure (ICP) and papilledema. In addition, AZD4017 in combination with prednisolone participated in phase II clinical trials for patients with Iatrogenic Cushing's Disease. It was postulated that the adverse metabolic effects of prednisolone could be reduced by co-administration of AZD4017.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| The metabolic syndrome. | 2005 Apr 16-22 |
|
| Glucocorticoids and cardiovascular disease. | 2007 Nov |
|
| Glucocorticoids and 11beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic syndrome. | 2007 Sep |
|
| Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017). | 2012 Jun 28 |
Patents
Sample Use Guides
Idiopathic intracranial hypertension: 400 mg of AZD4017 or placebo twice daily
Iatrogenic Cushing's Disease: AZD4017 will be given together with prednisolone 20mg daily for 7 days to compare its effects on metabolic tissues against the placebo arm where the participants will take placebo and prednisolone 20mg daily for 7 days
Route of Administration:
Oral
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DB14875
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C148516
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DTXSID80145044
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1024033-43-9
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ACTIVE MOIETY
