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  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)

Fadrozole (INN Tooltip 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.

References

1. 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.
2. 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. Archived from the original on April 15, 2013.