Entry Type
Name
Value
Parent Entry
Pharmacology Data Field
Reported as weakly effective to effective agonist.
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
Antagonist
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
Agonist
Levonorgestrel (API)
Pharmacology Data Field
No activity
Nestorone (API)
Pharmacology Data Field
Antagonist
Nestorone (API)
Pharmacology Data Field
Binds to GR but does not show activity in in vivo assays
Nestorone (API)
Pharmacology Data Field
No activity
Nestorone (API)
Pharmacology Data Field
No activity
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
No activity
Medroxyprogesterone Acetate (API)
Physical & Chemical Properties Data Field
214-215° C
Nomegestrol Acetate (API)
Physical & Chemical Properties Data Field
-62.6 in absolute ethanol at 22° C; -60 to -64 in absolute ethanol at 25° C
Nomegestrol Acetate (API)
Pharmacology Data Field
Binds but no agonist activity. "Weak," "partial" or "moderate" antagonist.
Nomegestrol Acetate (API)
Pharmacology Data Field
Antagonist
Nomegestrol Acetate (API)
Pharmacology Data Field
No activity
Nomegestrol Acetate (API)
Pharmacology Data Field
No activity
Nomegestrol Acetate (API)
Pharmacology Data Field
63-65%
Nomegestrol Acetate (API)
Pharmacology Data Field
98% bound to serum albumin
Nomegestrol Acetate (API)
Pharmacology Data Field
CYP3A3, CYP3A4, CYP2A6
Nomegestrol Acetate (API)
Toxicology Data Field
Abnormal bleeding/spotting, headache, hot flushes
Nomegestrol Acetate (API)
Pharmacology Data Field
Antagonist (40% of CPA, the most potent anti-androgenic progestin)
Dienogest (API)
Pharmacology Data Field
Weak or no agonist and antagonist activity
Dienogest (API)
Pharmacology Data Field
Low to no activity
Dienogest (API)
Pharmacology Data Field
No activity
Dienogest (API)
Pharmacology Data Field
Partial antagonist (about 30% activity of cyproterone acetate)
Drospirenone (API)
Pharmacology Data Field
Antagonist
Drospirenone (API)
Pharmacology Data Field
No activity
Drospirenone (API)
Pharmacology Data Field
Antagonist (antimineralocorticoid or aldosterone antagonist). Agonist reports vary: "weak" (Africander) to "strong" (Bartsch).
Drospirenone (API)
Pharmacology Data Field
Antagonist
Levonorgestrel (API)
Pharmacology Data Field
Conflicting reports: not active (Ruan, Lello), weakly effective (Nath), active (Bartsch), binds to GR (Jordan), low affinity (Africander)
Levonorgestrel (API)
Pharmacology Data Field
Agonist with high relative binding affinity. Conflicting reports on antagonism: Ruan and Lello indicate not active, while Africander says some anti-mineralocorticoid activity in rat models.
Levonorgestrel (API)
Toxicology Data Field
Generally very well tolerated, positive safety profile
Nomegestrol Acetate (API)
Pharmacology Data Field
Listed as "weak" (Jordan) and "active" (Ruan, Lello) agonist.
Etonogestrel (API)
Pharmacology Data Field
Antagonist
Etonogestrel (API)
Pharmacology Data Field
Reports vary: "weak" (Kuhl), "active" (Bartsch), "not active" (Ruan, Lello)
Etonogestrel (API)
Pharmacology Data Field
No activity
Etonogestrel (API)
Pharmacology Data Field
Reported as agonist with high relative binding affinity and no antagonist activity, but Stanczyk notes that data consistent with low androgenic potential and strong antagonist effects demonstrated in vitro.
Gestodene (API)
Pharmacology Data Field
Antagonist
Gestodene (API)
Pharmacology Data Field
Reported as "weak" (Africander, Kuhl) and "active" (Ruan, Lello) agonist
Gestodene (API)
Pharmacology Data Field
Binds. Activity reports vary slightly: reported as an antagonist (Ruan, Lello, Kuhl), while Africander reports that some antagonist activity is seen in rat models and Stanczyk claims it to be relatively weak compared to progesterone.
Gestodene (API)
Pharmacology Data Field
Agonist
Norethindrone (API)
Pharmacology Data Field
Agonist and antagonist
Norethindrone (API)
Pharmacology Data Field
No activity
Norethindrone (API)
Pharmacology Data Field
No activity
Norethindrone (API)
Pharmacology Data Field
Reports vary: "minimal androgenic activity" (Phillips), agonist (Ruan, Lello), partial agonist (DrugBank).
Norgestimate (API)
Pharmacology Data Field
Antagonist (Ruan, Lello). Selective agonist for ERα (Paris).
Norgestimate (API)
Pharmacology Data Field
Pronounced as "unknown" by Stanczyk in 2013, but previously claimed as not active (Ruan, Lello). Recently (2015) defined as full antagonist with low affinity (Paris).
Norgestimate (API)
Pharmacology Data Field
Varies: Full antagonist with moderate activity (Paris). No activity (Ruan, Lello).
Norgestimate (API)
Pharmacology Data Field
1.5-2 h, 2-3 h regardless of dose
Nomegestrol Acetate (API)
Pharmacology Data Field
Antagonist
Chlormadinone Acetate (API)
Pharmacology Data Field
Antagonist
Chlormadinone Acetate (API)
Pharmacology Data Field
Agonist
Chlormadinone Acetate (API)
Pharmacology Data Field
No activity
Chlormadinone Acetate (API)
Pharmacology Data Field
Potent antagonist
Cyproterone Acetate (API)
Pharmacology Data Field
Antagonist
Cyproterone Acetate (API)
Pharmacology Data Field
Agonist
Cyproterone Acetate (API)
Pharmacology Data Field
No activity
Cyproterone Acetate (API)
Pharmacology Data Field
Antagonist
Progesterone (API)
Pharmacology Data Field
Antagonist
Progesterone (API)
Pharmacology Data Field
"weak partial agonist" (Africander, Hapgood), activates GR "minimally" (Turgeon), "active" (Ruan, Lello)
Progesterone (API)
Pharmacology Data Field
"weak partial agonist" (Africander), active agonist (Bartsch). Antagonist.
Progesterone (API)