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Chemical compound
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]
Pharmacodynamics of aromatase inhibitors
Generation
Medication
Dosage
% inhibitiona
Classb
IC50 c
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
^ 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 ]
Estrogens
ER Tooltip Estrogen receptor agonists
Steroidal:
Alfatradiol
Certain
androgens /
anabolic steroids (e.g.,
testosterone ,
testosterone esters ,
methyltestosterone ,
metandienone ,
nandrolone esters ) (via estrogenic metabolites)
Certain
progestins (e.g.,
norethisterone ,
noretynodrel ,
etynodiol diacetate ,
tibolone )
Clomestrone
Cloxestradiol acetate
Conjugated estriol
Conjugated estrogens
Epiestriol
Epimestrol
Esterified estrogens
Estetrol †
Estradiol
Estradiol esters (e.g.,
estradiol acetate ,
estradiol benzoate ,
estradiol cypionate ,
estradiol enanthate ,
estradiol undecylate ,
estradiol valerate ,
polyestradiol phosphate ,
estradiol ester mixtures (
Climacteron ))
Estramustine phosphate
Estriol
Estriol esters (e.g.,
estriol succinate ,
polyestriol phosphate )
Estrogenic substances
Estrone
Estrone esters
Ethinylestradiol #
Hydroxyestrone diacetate
Mestranol
Methylestradiol
Moxestrol
Nilestriol
Prasterone (dehydroepiandrosterone; DHEA)
Promestriene
Quinestradol
Quinestrol
Progonadotropins
Antiestrogens
ER Tooltip Estrogen receptor antagonists (incl.
SERMs Tooltip selective estrogen receptor modulators /
SERDs Tooltip selective estrogen receptor downregulators )
Aromatase inhibitors
Antigonadotropins
Androgens /
anabolic steroids (e.g.,
testosterone ,
testosterone esters ,
nandrolone esters ,
oxandrolone ,
fluoxymesterone )
D2 receptor
antagonists (
prolactin releasers) (e.g.,
domperidone ,
metoclopramide ,
risperidone ,
haloperidol ,
chlorpromazine ,
sulpiride )
GnRH agonists (e.g.,
leuprorelin ,
goserelin )
GnRH antagonists (e.g.,
cetrorelix ,
elagolix )
Progestogens (e.g.,
chlormadinone acetate ,
cyproterone acetate ,
gestonorone caproate ,
hydroxyprogesterone caproate ,
medroxyprogesterone acetate ,
megestrol acetate )
Others