Fadrozole

Fadrozole
Clinical data
Trade names	Afema
Routes of; administration	By mouth
Drug class	Aromatase inhibitor;Antiestrogen
ATC code	None;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile;
CAS Number	102676-47-1; hydrochloride:102676-31-3;
PubChemCID	59693;
ChemSpider	53850;
UNII	H3988M64PU; hydrochloride:H0Q44H4ECQ;
KEGG	D02451;
ChEMBL	ChEMBL9298;
CompTox Dashboard(EPA)	DTXSID5034141;
Chemical and physical data
Formula	C14H13N3
Molar mass	223.279g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CC(N2C=NC=C2C1)C3=CC=C(C=C3)C#N;
	InChI InChI=1S/C14H13N3/c15-8-11-4-6-12(7-5-11)14-3-1-2-13-9-16-10-17(13)14/h4-7,9-10,14H,1-3H2; Key:CLPFFLWZZBQMAO-UHFFFAOYSA-N;
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Fadrozole(INNTooltip International Nonproprietary Name), sold under the brand nameAfema(byNovartis), is aselective,nonsteroidal aromatase inhibitorwhich is or has been used inJapanfor the treatment ofbreast cancer.^[1]^[2]

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Pharmacodynamics of aromatase inhibitors
Generation	Medication	Dosage	% inhibition^a	Class^b	IC₅₀^c
First	Testolactone	250 mg 4x/dayp.o.	?	Type I	?
	Testolactone	100 mg 3x/weeki.m.	?	Type I	?
	Rogletimide	200 mg 2x/dayp.o. 400 mg 2x/dayp.o. 800 mg 2x/dayp.o.	50.6% 63.5% 73.8%	Type II	?
	Aminoglutethimide	250 mg mg 4x/dayp.o.	90.6%	Type II	4,500 nM
Second	Formestane	125 mg 1x/dayp.o. 125 mg 2x/dayp.o. 250 mg 1x/dayp.o.	72.3% 70.0% 57.3%	Type I	30 nM
	Formestane	250 mg 1x/2 weeksi.m. 500 mg 1x/2 weeksi.m. 500 mg 1x/1 weeki.m.	84.8% 91.9% 92.5%	Type I	30 nM
	Fadrozole	1 mg 1x/dayp.o. 2 mg 2x/dayp.o.	82.4% 92.6%	Type II	?
Third	Exemestane	25 mg 1x/dayp.o.	97.9%	Type I	15 nM
	Anastrozole	1 mg 1x/dayp.o. 10 mg 1x/dayp.o.	96.7–97.3% 98.1%	Type II	10 nM
	Letrozole	0.5 mg 1x/dayp.o. 2.5 mg 1x/dayp.o.	98.4% 98.9%–>99.1%	Type II	2.5 nM
Footnotes:^a= Inpostmenopausalwomen.^b= Type I:Steroidal,irreversible(substrate-binding site). Type II:Nonsteroidal,reversible(binding to and interference with thecytochrome P450 heme moiety).^c= Inbreast cancer homogenates.Sources:See template.

References[edit]

^Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A (February 1991). "Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease".J. Med. Chem.34(2): 725–36.doi:10.1021/jm00106a038.PMID 1825337.
^Raats JI, Falkson G, Falkson HC (January 1992)."A study of fadrozole, a new aromatase inhibitor, in postmenopausal women with advanced metastatic breast cancer".J. Clin. Oncol.10(1): 111–6.doi:10.1200/jco.1992.10.1.111.PMID 1530798.^{[permanent dead link]}