Fadrozole information

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 ;
PubChem CID	59693;
ChemSpider	53850 ;
UNII	H3988M64PU; hydrochloride: H0Q44H4ECQ ;
KEGG	D02451 ;
ChEMBL	ChEMBL9298 ;
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 ; Key:CLPFFLWZZBQMAO-UHFFFAOYSA-N ;
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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	% inhibition^a	Class^b	IC₅₀^c
First	Testolactone	250 mg 4x/day p.o.	?	Type I	?
	Testolactone	100 mg 3x/week i.m.	?	Type I	?
	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
	Formestane	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%	Type I	30 nM
	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.

^ 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]}

[pmid1825337-1] 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.

[pmid1530798-2] 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.^{[permanent dead link]}

Fadrozole information

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Fadrozole

Aromatase inhibitor

Anastrozole

Non steroidal aromatase inhibitors

Estrogen

Letrozole

Hormone therapy

Norethisterone

Transgender hormone therapy

Diethylstilbestrol

Hormone replacement therapy

Exemestane

Nitrile

Feminizing hormone therapy

Antiestrogen

Tibolone

Pharmacokinetics of estradiol

Vaginal estrogen

Megestrol acetate

Estradiol valerate

Ormeloxifene

Bioidentical hormone replacement therapy

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
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