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Trilostane
Systematic (IUPAC) name
(4α,5α,17β)-3,17-dihydroxy-4,5-epoxyandrost-2-ene-2-carbonitrile
Identifiers
CAS number 13647-35-3
ATC code H02CA01
PubChem 656583
DrugBank APRD01276
Chemical data
Formula C 20H27NO3  
Mol. mass 329.433 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 8 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status Withdrawn (U.S.)
Routes  ?

Trilostane is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.[1]

It is perhaps best known under the trade name Vetoril. It was withdrawn from the United States market in April 1994. However, it was recently approved in 2008 for the treatment of Cushing's disease (hyperandrenocorticism) in dogs.[2]

It is also the first drug approved to treat both pituitary- and adrenal-dependent Cushing's in dogs. This prescription drug works by stopping the production of cortisol in the adrenal glands. In studies of the drug, the most common side effects were vomiting, lack of energy, diarrhea, and weight loss. Trilostane should not be given to a dog that:

  1. has kidney or liver disease;
  2. takes certain medications used to treat heart disease; or
  3. is pregnant

The safety and effectiveness of trilostane were shown in several studies. Success was measured by improvements in both blood test results and physical symptoms (increased appetite and activity level, and decreased panting, thirst and urination).

Only one other drug, Anipryl (selegiline), is FDA-approved to treat Cushing's disease in dogs, but only to treat uncomplicated, pituitary-dependent Cushing's. [3]

It has been used as a progesterone inhibitor.[4]

A number of compounding pharmacies in the US sell the product, although it is not approved for use. FDA's enforcement discretion makes action unlikely.

Chemistry

The compound is prepared from testosterone in a four step synthesis.

References

  1. ^ Komanicky P, Spark RF, Melby JC. (1978). "Treatment of Cushing's syndrome with trilostane (WIN 24,540), an inhibitor of adrenal steroid biosynthesis". Journal of Clinical Endocrinology and Metabolism 47 (5): 1042–1051. PMID 233687.  
  2. ^ http://www.fda.gov/consumer/updates/cushings051109.html
  3. ^ http://www.fda.gov/consumer/updates/cushings051109.html
  4. ^ le Roux PA, Tregoning SK, Zinn PM, van der Spuy ZM (June 2002). "Inhibition of progesterone secretion with trilostane for mid-trimester termination of pregnancy: randomized controlled trials". Human reproduction (Oxford, England) 17 (6): 1483–9. doi:10.1093/humrep/17.6.1483. PMID 12042266. http://humrep.oxfordjournals.org/cgi/pmidlookup?view=long&pmid=12042266.  
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