Fadrozole

Fadrozole (INN), 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]

Pharmacodynamics of aromatase inhibitors
GenerationMedicationDosage % inhibitionaClassbIC50c
FirstTestolactone250 mg 4x/day p.o. ?Type I ?
100 mg 3x/week i.m. ?
Rogletimide200 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 ?
Aminoglutethimide250 mg mg 4x/day p.o.90.6%Type II4,500 nM
SecondFormestane125 mg 1x/day p.o.
125 mg 2x/day p.o.
250 mg 1x/day p.o.
72.3%
70.0%
57.3%
Type I30 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%
Fadrozole1 mg 1x/day p.o.
2 mg 2x/day p.o.
82.4%
92.6%
Type II ?
ThirdExemestane25 mg 1x/day p.o.97.9%Type I15 nM
Anastrozole1 mg 1x/day p.o.
10 mg 1x/day p.o.
96.7–97.3%
98.1%
Type II10 nM
Letrozole0.5 mg 1x/day p.o.
2.5 mg 1x/day p.o.
98.4%
98.9%–>99.1%
Type II2.5 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 namesAfema
Routes of
administration
By mouth
Drug classAromatase 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
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC14H13N3
Molar mass223.279 g·mol−1
3D model (JSmol)
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)

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.


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