May also decrease levels of androgen receptor in addition to other mechanisms.
What is Bicalutamide?
100
Inhibits non-ovarian and ovarian aromatase?
What is Letrazole?
(Femara)
100
Osteoporosis
What is Exemestane (& Anastrazole & Letrazole)?
100
This property causes these drugs to have less off-target effects than another in its class, Exemestane.
What is non-steroidal.
200
Covalently binds to CYP17A1.
What is Abiratarone Acetate (& Ketaconazole)?
200
Prevents translocation of AR to nucleus, if translocation occurs, AR cannot respont correctly with response elements to transcribe mRNA, and decreases levels of AR.
What is MDV3100?
200
Fluid retention, CHF, HTN, cataracts w/ long time use
What are Glucocorticoids?
200
Testosterone is convered to this by CYP19A1
What is estradiol?
300
binds to the ER receptor and prevents translocation, if complex does translocate, proper transcription does not occur.
What is Tamoxifen (& Toremifene)?
300
Irreversibly inhibits CYP19A1.
What is Exemestane?
300
HTN
What is Abiraterone Acetate?
300
Metabolized by CYP2C8 & 3A4
What is Enzalutamide?
300
Activate Tamoxifen to the very active metabolite, Endoxifen.
What is CYP3A4 & 2D6?
(demethylation) & (hydroxlyation)
400
Prevents translocation and proper transcription like other ER antagonists, but also down regulation and destruction of the receptor.
( What is Fulvestrant? )
400
anti-cancer, anti-emetic and comfort properties
What are Glucocorticoids?
400
Seizures
(asthenia, arthralgia, diarrhea & HTN)
What is MDV3100?
or
What is Enzalutamide?
400
Positive food effect that can effect elderly men with compromised heart function
What is Abiraterone acetate?
500
Binds to the androgen receptor, prevents translocation into the nucleus.
What is Bicalutamide (Flutamide, Nilutamide)?
500
Reversibly inhibit CYP19A1 (aromatase).
What is Anastrazole & Letrazole?
500
Secondary endometrial cancer
What is Tamoxifen?
500
Less lung and liver toxicity than earlier drugs in its class.
What is Bicalutamide?
(The nitrile group instead of nitro group prevents targeting by reductase enzyme, unlike Flutamide, Nilutamide)
500
Antiestrogens can only be use in this breast cancer population
What is ER+ breast cancer in postmenapausal women?