|
Proprietary Name: |
ERLEADA (Active
Ingredient: Apalutamide) |
|
API |
Apalutamide |
|
Dosage Form: |
Tablet |
|
Strength: |
60 mg, 240 mg |
|
Daily Dose: |
240 mg
administered orally once daily. |
|
Ingredients: |
colloidal
anhydrous silica, croscarmellose sodium, hydroxypropyl
methylcellulose-acetate succinate, silicified microcrystalline cellulose, and
magnesium stearate |
|
Appl. No. |
N210951 |
|
Route, dosage: |
Oral |
|
Supply: |
240 mg: 30 tablets
/ bottle; 60 mg: 120 tablets / bottle |
|
Appl. Holder |
Janssen Biotech
Inc. |
|
Indications: |
Metastatic
castration-sensitive prostate cancer (mCSPC) Non-metastatic
castration-resistant prostate cancer (nmCRPC) |
|
Mechanism: |
an Androgen
Receptor (AR) inhibitor that binds directly to the ligand-binding domain of
the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding,
and impedes AR-mediated transcription. Major metabolite: N-desmethyl
apalutamide |
|
Parameter(s) |
Value(s) |
|
Absolute Bioavailability |
~100% |
|
Tmax, h |
2 (1-5) |
|
Effect of Food |
Tmax +2h; no effect to Cmax and AUC |
|
T1/2, day(s) |
3 |
|
Metabolism |
Metabolized by CYP2C8 and CYP3A4 to form N-desmethyl apalutamide. |
|
Excretion |
24% in feces and 65% in urine |
|
Patent No |
Patent Expiration |
Key Claim Elements |
|
8445507 |
09/15/2030 |
Chemical Structure
of apalutamide. |
|
8802689 |
03/27/2027 |
A method for
treating a disease related to nuclear receptor activity. |
|
9388159 |
03/27/2027 |
Chemical |
|
9987261 |
03/27/2027 |
A capsule/tablet
comprising a compound … |
|
9481663 |
06/04/2033 |
A crystalline Form
B |
|
9884054 |
09/23/2033 |
A method of
treating non-metastatic castration-resistant prostate cancer
in a male human |
|
09/23/2033 |
A method of
treating a male human with non-metastatic castration-resistant
prostate cancer, the method |
|
|
09/23/2033 |
A method of
treating non-metastatic castration-resistant prostate cancer
in a male human |
|
|
04/30/2038 |
A method of
improving metastasis free survival in a male human with nonmetastatic castration-resistant
prostate cancer …. apalutamide in combination with androgen deprivation
therapy |
|
US 20220324831 A1 |
Form Y, Olon SpA, (Pending) |
|
US 20220281836 A1 |
Form unknown with Peaks at 12.1°, 16.0°, 16.7°,
20.1°20.3°±0.1°2θ, Dr. Reddys, (Pending) |
|
US 20220153718 A1 |
Amorphous form, Olon SpA, (Pending) |
|
US 20220073472 A1 |
Amorphous form + a drug, ESSA Pharma Inc., (Granted;
Expire Date: 2041-04-16) |
|
US 20190322640 A1 US 11149017 B2 |
Forms T13, T11, T2, T6*, Teva, (Granted; Expire Date:
2037-12-13) Forms T13, T11, T2, Teva, (Granted; Expire Date:
2037-12-13) (App# US16/468,912) |
|
US 9481663B2 |
Form B, OB patent. Its description mentions Form A-Form
J. (Exp. Date: 2033-06-04) |
|
Claim 1 Form with Peaks at 7.7±0.1° 2-Theta, 10.4±0.1°
2-Theta, 11.6±0.1° 2-Theta, 17.0±0.1° 2-Theta, 20.0±0.1° 2-Theta, and
20.6±0.1° 2-Theta. Aragon Pharma. (App# US15/975,449; Exp. Date: 2033-06-04)
Its description mentions Form A-Form J. |
|
|
Only CN filing. 苏州晶云药物 Form
I: 16.7 ° ± 0.2 °, 20.4 ° ± 0.2 °, and 12.1 ° ± 0.2 Form II: Peaks at 14.4° ± 0.2°, 16.6° ± 0.2°, 17.9 ° ±
0.2°. (Publish Date: 2016-08-11) |
|
|
No national filings. Cipla, Claims C2 to C10. (Publish
Date: 2020-03-12) |
|
|
No national filings. Laurus Labs. Claims L2, L1 and
amorphous. Its description mentions L3 - L14. (Publish Date: 2020-11-26) |
