Fadrozole

Fadrozole (INNTooltip International Nonproprietary Name), sold under the brand name Afema (by Novartis), is a selective, nonsteroidal aromatase inhibitor which is or has been used in Japan for the treatment of breast cancer.^[1][2]

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Pharmacodynamics of aromatase inhibitors

Generation	Medication	Dosage	% inhibitiona	Classb	IC50c
First	Testolactone	250 mg 4x/day p.o.	?	Type I	?
		100 mg 3x/week i.m.	?
	Rogletimide	200 mg 2x/day p.o. 400 mg 2x/day p.o. 800 mg 2x/day p.o.	50.6% 63.5% 73.8%	Type II	?
	Aminoglutethimide	250 mg mg 4x/day p.o.	90.6%	Type II	4,500 nM
Second	Formestane	125 mg 1x/day p.o. 125 mg 2x/day p.o. 250 mg 1x/day p.o.	72.3% 70.0% 57.3%	Type I	30 nM
		250 mg 1x/2 weeks i.m. 500 mg 1x/2 weeks i.m. 500 mg 1x/1 week i.m.	84.8% 91.9% 92.5%
	Fadrozole	1 mg 1x/day p.o. 2 mg 2x/day p.o.	82.4% 92.6%	Type II	?
Third	Exemestane	25 mg 1x/day p.o.	97.9%	Type I	15 nM
	Anastrozole	1 mg 1x/day p.o. 10 mg 1x/day p.o.	96.7–97.3% 98.1%	Type II	10 nM
	Letrozole	0.5 mg 1x/day p.o. 2.5 mg 1x/day p.o.	98.4% 98.9%–>99.1%	Type II	2.5 nM
Footnotes: a = In postmenopausal women. b = Type I: Steroidal, irreversible (substrate-binding site). Type II: Nonsteroidal, reversible (binding to and interference with the cytochrome P450 heme moiety). c = In breast cancer homogenates. Sources: See template.

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 Y hydrochloride: 102676-31-3 Y
PubChem CID	59693
ChemSpider	53850 N
UNII	H3988M64PU hydrochloride: H0Q44H4ECQ Y
KEGG	D02451 Y
ChEMBL	ChEMBL9298 N
CompTox Dashboard (EPA)	DTXSID5034141
Chemical and physical data
Formula	C14H13N3
Molar mass	223.279 g·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 N Key:CLPFFLWZZBQMAO-UHFFFAOYSA-N N
NY (what is this?)  (verify)