Dutasteride
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Dutasteride
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| Systematic (IUPAC) name | |
| (5α, 17β)-N-{2,5 bis(trifluoromethyl) phenyl}-3-oxo-4-azaandrost-1-ene-17-carboxamide | |
| Identifiers | |
| CAS number | |
| ATC code | G04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C27H30F6N2O2 |
| Mol. mass | 528.53 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 60% |
| Protein binding | 99% |
| Metabolism | Hepatic (CYP3A4-mediated) |
| Half life | 5 weeks |
| Excretion | Fecal |
| Therapeutic considerations | |
| Pregnancy cat. |
X(US) Not to be handled by pregnant women |
| Legal status | |
| Routes | Oral |
Dutasteride (marketed as Avodart, Avidart, Avolve, Duagen, Dutas, Dutagen, Duprost) is a 5-alpha-reductase inhibitor, a drug which inhibits the conversion of testosterone into dihydrotestosterone (DHT). It is used to treat conditions caused by DHT, such as benign prostatic hyperplasia (BPH).
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[edit] Classification and Method of Action
Dutasteride belongs to a class of drugs called 5-alpha-reductase inhibitors, which block the action of the 5-alpha-reductase enzymes that convert testosterone into dihydrotestosterone (DHT). Finasteride also belongs to this group. Dutasteride inhibits both isoforms of 5-alpha reductase, while finasteride inhibits only one. But a clinical study done by GlaxoSmithKline, the EPICS trial, did not find dutasteride to be more effective than finasteride in treating BPH.
[edit] Uses
While dutasteride is officially approved to treat enlargement of the prostate gland, Clinical trials for dutasteride as a hair loss drug were undertaken, but called off in late 2002. The reason the trials were called off is not publicly known. Industry sources speculate that Avodart would have been seen as too similar to Propecia to have proved profitable as a hair loss treatment. However, phase II results indicated that dutasteride 2.5mg generated a superior hair count to finasteride 5mg at 12 and 24 weeks.[1]
In December 2006, Avodart manufacturer GlaxoSmithKline embarked on a new Phase III, six month study in Korea to test the safety, tolerability and effectiveness of a once-daily dose of dutasteride (0.5mg) for the treatment of male pattern baldness in the vertex region of the scalp (types IIIv, IV and V on the Hamilton-Norwood scale).[2] The future impact that this study will have on the FDA's approval or disapproval of Avodart for the treatment of male pattern baldness in the United States is yet to be determined.
Dutasteride is also in development for Prostate cancer risk reduction.[3]
[edit] Teratogenic effect
The teratogenic effect from Dutasteride is a very large risk for male children. The effect would be identical to 5-alpha-reductase deficiency, where a developing male child naturally is deficient in 5-alpha reductase, and thus unable to synthesize DHT. As Dutasteride blocks the same process, a developing male would have this deficiency as a result of medication, rather than simply naturally.
[edit] See also
[edit] External links
- Effectiveness of Dutasteride as a treatment for Male Pattern Baldness, as reported by Science Daily.
- Official site
- http://www.hairlosshelp.com/html/Dutasteride_hair_loss_trials.cfm
[edit] References
- ^ The importance of dual 5alpha-reductase inhibition...[J Am Acad Dermatol. 2006] - PubMed Result
- ^ ClinicalTrials.gov NCT00441116
- ^ Sound bites for NCE Entries into Phase III
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