Steroids and Derivatives

Impurity Atorvastatin 2-Hydroxy Lactone
Stability Hygroscopic
Applications A metabolite of Atorvastatin, a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia.

Stability Not stable in Acidic or basic condition
Applications 6β-Methyl Fluorometholone is an impurity in the synthesis of Fluorometholone (F593145), a glucocorticoid; anti-inflammatory.
References Kupferman, A., et al.: Arch. Ophthlmol., 640, 100 (1982), Tokunaga H., et al.: Chem. Pharm. Bull., 32, 4012 (1984),

Applications Glucocorticoid.

Stability Light Sensitive, Temperature Sensitive
Applications An Atorvastatin (A791750) derivative which have improved stability.

Applications Testosterone Isocaproate, is one of the common anabolic steroid esters. It is a controlled substance in US due to their potential for abuse and misuse. It can be used for the treatment of constitutional delayed puberty (CDP), in combination of other testosterone esters.
References Noggie, F. T., et al.: J. Chromatography. Sci., 28 (5), 263 (1990); Buyukgebiz, A., et al.: Hormone REs., 44 Suppl 3, 32 (1995);

Applications (6α,9β,11β,16α)-21-(Acetyloxy)-9,11-epoxy-6-fluoro-17-hydroxy-16-methylpregna-1,4-diene-3,20-dione is an intermediate in the synthesis of Paramethasone Acetate (P191845), a derivative of Dexamethasone (D298800), a potent synthetic member of the glucocorticoid class of steroid drugs that has anti-inflammatory and immunosuppressant properties.
References Wershil, B.K., et al.: Int. Arch. Allergy Immunol., 107, 323 (1995), Riccardi, C., et al.: Cell Death Diff., 6, 1182 (1999), Llanos, S.L. and Roldan, A.: Bio Cell, 23, 29 (1999)

Applications Mexrenone is an impurity of eplerenon (E588775). Eplerenone is a selective aldosterone receptor antagonist (SARA), structurally similar to Spiranolactone. Eplerenone is used alone or in combination with other medications to treat high blood pressure. Eplerenone is in a class of medications called mineralocorticoid receptor antagonists. It works by blocking the action of aldosterone, a natural substance in the body that raises blood pressure.
References de Gasparo, M., et al.: J. Pharmacol. Exp. Ther., 240, 650 (1987), Delyani, J.A., et al.: Cardiovasc. Drug Rev., 19, 185 (2001), Burgess, E., et al.: Expert. Opin. Pharmacother., 5, 2573 (2004), Ravis, W.R., et al.: J. Clin. Pharmacol., 45, 810 (2005),

Applications A labelled metabolite of Equilin (E592800).
References Enmark, E., et al.: J. Clin. Endocrinol. Metab., 82, 4258 (1997), Wang, Z., et al.: J. Med. Chem., 43, 2419 (2000), Jiang, X., et al.: Steroids, 71, 334 (2006),

Applications N-Des(1,1-dimethylethyl) N-Cyclohexyl Finasteride is an impurity of Finasteride (F342000); an inhibitor of 5α-reductase which is the enzyme that converts testosterone to the more potent androgen 5α-dihydrotestosterone.Also an antialopecia agent.
References Koronkowski, M.J., et al.: Pharmacotherapy, 13, 309 (1993); Tenover, J.L., et al.: Clin. Ther., 19, 243 (1997); McConnell, J.D., et al.: N. Engl. J. Med., 338, 557 (1998)

Applications Dexamethasone Acetate Impurity E is a pregn-4-ene derivative used in the preparation of antiallergic and antiinflammatory drugs.
References Nedelec, L., et al.: Ger. Offen. (1978)

Applications Atorvastatin-d5 tert-Butyl Ester is the labeled analogue of Atorvastatin tert-Butyl Ester (A791740), an impurity arising in the synthesis of Atorvastatin (A791750), a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia.
References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993); Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996); Whitfield, L.R., et al.: Eur. J. Drug Metab. Pharmacokinet., 25, 97 (2000)

Applications 6-Ethylchenodeoxycholic-d5 Acid is an isotope labelled compound of 6-Ethylchenodeoxycholic Acid (E899810), which is used in the investigative treatment of primary biliary cholangitis. Primary biliary cholangitis is an autoimmune disease of the liver that slowly progresses to cirrhosis.
References Ali, A. H, et al.: Expert Opin. Orphan Drugs, 4, 1011 (2016)

Applications 21-Butyryloxy Budesonide is a derivative of Budesonide (B689490), a non-halogenated glucocorticoid related to triamcinolone hexacetonide.
References Ryrfeldt., A., et a.: J. Steroid Biochem., 10, 317 (1979); Roth, G., et al.: J. Pharm. Sci., 69, 766 (1980); Clissold, S.P., et al.: Drugs, 28, 485 (1984)

Applications 16α-Hydroxypregna-4,9(11)-diene-3,20-dione is an intermediate in the synthesis of 16-Hydroxycorticosterone 20-Hydroxy-21-Acid (H918430), an oxidized derivative of corticosterone (C695700).
References Allen, G.R., et al.: J. Am. Chem. Soc., 81, 4968 (1959);

Applications 23-Hydroxybudesonide is an metabolite of budesonide (B689490), a non-halogenated glucocorticoid related to triamcinolone hexacetonide. Used as an antiinflammatory agent.
References Edsbaecker, S., et al.: Drug. Metabol. Dispostion., 15, 403 (1987); Moore, C.D., et al.: Drug. Metabolism. Disposition., 41, 379 (2013);

Applications Controlled substance.