APALUTAMIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H15F4N5O2S
Molecular Weight	477.435
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CNC(=O)C1=CC=C(C=C1F)N2C(=S)N(C(=O)C23CCC3)C4=CC(=C(N=C4)C#N)C(F)(F)F

InChI

InChIKey=HJBWBFZLDZWPHF-UHFFFAOYSA-N

InChI=1S/C21H15F4N5O2S/c1-27-17(31)13-4-3-11(8-15(13)22)30-19(33)29(18(32)20(30)5-2-6-20)12-7-14(21(23,24)25)16(9-26)28-10-12/h3-4,7-8,10H,2,5-6H2,1H3,(H,27,31)

HIDE SMILES / InChI

Molecular Formula	C21H15F4N5O2S
Molecular Weight	477.435
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://adisinsight.springer.com/drugs/800032695
Curator's Comment: Description was created based on several sources, including https://newdrugapprovals.org/2016/03/11/18141/ https://www.ncbi.nlm.nih.gov/pubmed/22266222

Apalutamide (developmental code name ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment. Apalutamide binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. Apalutamide is currently in phase III clinical trials for castration-resistant prostate cancer.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Androgen Receptor 167 Target ID: CHEMBL1871 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22266222	Antagonist 2778		16.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Prostate cancer 178 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	Primary		Approved 8429	ERLEADA Approved Use ERLEADA is an androgen receptor inhibitor indicated for the treatment of patients with non-metastatic castration-resistant prostate cancer. Launch Date 2018

C_max

Value	Dose	Co-administered	Analyte	Population
6 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		APALUTAMIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
100 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		APALUTAMIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
72 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		APALUTAMIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
4% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		APALUTAMIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
480 mg 1 times / day multiple, oral Highest studied dose Dose: 480 mg, 1 times / day Route: oral Route: multiple Dose: 480 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24002508	unhealthy, 68 years (range: 45 - 81 yers) n = 3 Health Status: unhealthy Condition: castration-resistant prostate cancer Age Group: 68 years (range: 45 - 81 yers) Sex: M Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/24002508	Sources: https://pubmed.ncbi.nlm.nih.gov/24002508
300 mg 1 times / day multiple, oral Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24002508	unhealthy, 68 years (range: 45 - 81 yers) n = 5 Health Status: unhealthy Condition: castration-resistant prostate cancer Age Group: 68 years (range: 45 - 81 yers) Sex: M Population Size: 5 Sources: https://pubmed.ncbi.nlm.nih.gov/24002508	DLT: Abdominal pain... Dose limiting toxicities: Abdominal pain (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/24002508
240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	Disc. AE: Rash, Rash... AEs leading to discontinuation/dose reduction: Rash (3%) Rash (>1) Diarrhea (>1) Fatigue (>1) Nausea (>1) Vomiting (>1) Hypertension (>1) Hematuria (>1) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130	Disc. AE: Fatigue, Decreased appetite... AEs leading to discontinuation/dose reduction: Fatigue (1%) Decreased appetite (0.7%) Weight decreased (0.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130

AEs

AE	Significance	Dose	Population
Abdominal pain	grade 3, 1 patient DLT, Disc. AE	300 mg 1 times / day multiple, oral Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24002508	unhealthy, 68 years (range: 45 - 81 yers) n = 5 Health Status: unhealthy Condition: castration-resistant prostate cancer Age Group: 68 years (range: 45 - 81 yers) Sex: M Population Size: 5 Sources: https://pubmed.ncbi.nlm.nih.gov/24002508
Rash	3% Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
Diarrhea	>1 Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
Fatigue	>1 Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
Hematuria	>1 Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
Hypertension	>1 Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
Nausea	>1 Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
Rash	>1 Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
Vomiting	>1 Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf
Decreased appetite	0.7% Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130
Weight decreased	0.7% Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130
Fatigue	1% Disc. AE	240 mg 1 times / day steady, oral Recommended\|MTD Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130	unhealthy, 74 years (range: 48-97 years) n = 803 Health Status: unhealthy Age Group: 74 years (range: 48-97 years) Sex: M Population Size: 803 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf Page: p. 130

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inducer 781 inhibitor 1587	inhibitor 1767		inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B6 810 CYP2C19 1478 CYP2C8 911 P-gp 1461 BCRP 699 OCT2 647 OAT3 642 MATE1 306 MATE2 263	CYP2C8 693 P-gp 1537 carboxylesterase 4	CYP2B6 547 P-gp 257 OATP1B1 26 BCRP 75

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [IC50 12 uM]
MATE1 308	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [IC50 13.8 uM]
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [IC50 27.2 uM]
MATE2 263	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [IC50 37.9 uM]
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [IC50 4.8 uM]	N-desmethyl apalutamide 1
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [IC50 7.6 uM]	N-desmethyl apalutamide 1
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=205 Page: 205.0	yes [Ki 0.3 uM]
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 27 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 28 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 33.5 uM]
BCRP 773	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	N-desmethyl apalutamide 1
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	N-desmethyl apalutamide 1
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	N-desmethyl apalutamide 1
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	N-desmethyl apalutamide 1
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	N-desmethyl apalutamide 1
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	N-desmethyl apalutamide 1
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	N-desmethyl apalutamide 1
OATP1B1 803	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes
P-gp 1650	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes		yes (co-administration study) Comment: co-administration of apalutamide 240 QD with single oral doses of sensitive transporter substrates resulted in a 30% decrease in the AUC of fexofenadine (a P-gp substrate) and 41% decrease in the AUC of rosuvastatin (a BCRP/OATP1B1 substrate). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes		yes (co-administration study) Comment: co-administration of apalutamide 240 QD with single oral doses of sensitive transporter substrates resulted in a 30% decrease in the AUC of fexofenadine (a P-gp substrate) and 41% decrease in the AUC of rosuvastatin (a BCRP/OATP1B1 substrate). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	N-desmethyl apalutamide 1	yes (co-administration study) Comment: co-administration of apalutamide 240 QD with single oral doses of sensitive transporter substrates resulted in a 30% decrease in the AUC of fexofenadine (a P-gp substrate) and 41% decrease in the AUC of rosuvastatin (a BCRP/OATP1B1 substrate). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	major
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=65 Page: 65.0	yes
carboxylesterase 4	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes	yes (co-administration study) Comment: In a dedicated drug-interaction study 1012, concomitant itraconazole (a strong CYP3A4 inhibitor) decreased a single dose apalutamide's Cmax by 22 % without AUC change. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210951Orig1s000MultidisciplineR.pdf#page=38 Page: 38.0		N-desmethyl apalutamide 1

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY105300	https://www.001chemical.com/chem/956104-40-8
AA Blocks	AA00IJ5V	https://www.aablocks.com/goods/Goods/detail?id=AA00IJ5V
AK Scientific, Inc. (AKSCI)	Y0375	http://www.aksci.com/item_detail.php?cat=Y0375
Aaron Chemicals	AR00IJXN	http://www.aaronchem.com/956104-40-8
AbMole Bioscience	M2270	http://www.abmole.com/products/arn-509.html
Aceschem	ACF023740	https://www.aceschem.com/catalog/956104-40-8.html
Achemtek	0102-014226	http://www.achemtek.com/956104-40-8
Acorn PharmaTech	ACN-031562	http://www.acornpharmatech.com/
Active Biopharma	ABP001022	http://www.activebiopharma.com/956104-40-8
Adooq BioScience	A11923	https://www.adooq.com/arn-509.html
Ambinter	Amb22170037	http://www.ambinter.com/reference/22170037
Angel Pharmatech	AG-19820	http://www.angelpharmatech.com/956104-40-8.html
ApexBio Technology	A8364	http://www.apexbt.com/arn-509.html
Ark Pharm	AK174739	http://www.arkpharminc.com/products/956104-40-8.html
Ark Pharma Scientific Limited	A-0655	http://www.arkpharmtech.com/product/32606.html
Aurora Fine Chemicals LLC	A24.094.209	http://online.aurorafinechemicals.com/info?ID=A24.094.209
Aurora Fine Chemicals LLC	K16.648.661	http://online.aurorafinechemicals.com/info?ID=K16.648.661
Aurum Pharmatech LLC	W-5908	http://www.Aurumpharmatech.com/Product/ProductDetails/W_5908
Axon MedChem	1979	https://www.axonmedchem.com/product/1979
BOC Sciences	956104-40-8	https://www.bocsci.com/apalutamide-cas-956104-40-8-item-462663.html
BioChemPartner	BCP05829	http://www.biochempartner.com/956104-40-8-BCP05829
BioCrick	BCC3724	http://www.biocrick.com/ARN-509-BCC3724.html
BioSynth	J-519596	https://www.biosynth.com/en/products/all-products/products/J-519596.html
Boerchem	BC600521	http://www.boerchem.com/?product_43356.html
Chem Scene	CS-0885	http://www.chemscene.com/956104-40-8.html
ChemFish Tokyo co.,ltd	24872560	http://www.chemfish.co.jp/index.php?id=4626&project=product
Chemspace	CSSB00020668737	https://chem-space.com/CSSB00020668737
DAOGE BIOPHARMA	DG21-10659	https://www.daogechem.com/product/956104-40-8.html
DC Chemicals	DC7064	http://www.dcchemicals.com/product_show-Apalutamide_ARN509_.html
Excenen	EX-A089	http://www.excenen.com/searchresultlist.php?id=956104-40-8
Hairui	APCQ018	http://www.hairuichem.com/en/product/956104-40-8.html
Lab Network	LN01314169	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01314169
Matrix Scientific	124915	https://www.matrixscientific.com/124915.html
MedChem Express	HY-16060	https://www.medchemexpress.com/ARN-509.html
Molcore	MC105300	https://www.molcore.com/product/956104-40-8
MuseChem	I005661	https://www.musechem.com/product/I005661.html
Renno Tech	RL06020	http://www.rennotech.com/product_show.asp?id=6268
Sinfoo Biotech	S060967	http://www.sinfoobiotech.com/product/1064367
Smolecule	S548653	http://www.smolecule.com/products/s548653
Synblock Inc	PB27306	http://www.synblock.com/product/956104-40-8.html
THE BioTek	bt-288058	https://www.thebiotek.com/product/inhibitors/bt-288058
THE BioTek	bt-506182	https://www.thebiotek.com/product/others/bt-506182
TubePharm	Tube705	http://www.tubepharm.com/product/956104-40-8-en.html
abcr GmbH	AB479612	http://www.abcr.com/shop/en/AB479612
eNovation Chemicals	D371785	http://www.enovationchem.com/productDetails.asp?productID=D371785
eNovation Chemicals	D580228	https://www.enovationchem.com/ProductDetails.asp?ProductID=D580228
eNovation Chemicals	Y0974363	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0974363
iChemical	EBD2207159	http://www.ichemical.com/products/956104-40-8.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs

PubMed

Title	Date	PubMed
ARN-509: a novel antiandrogen for prostate cancer treatment.	2012 Mar 15	22266222
New agents for prostate cancer.	2014 Sep	24658665
Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort.	2016 Dec	27160947

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose of ERLEADA (apalutamide) is 240 mg (four 60 mg tablets) administered orally once daily. Swallow the tablets whole. ERLEADA can be taken with or without food.

Route of Administration: Oral

In Vitro Use Guide

APALUTAMIDE binds AR with IC50 16 nM

Substance Class	Chemical Created by `admin` on `Sat Dec 16 04:48:59 GMT 2023` Edited by `admin` on `Sat Dec 16 04:48:59 GMT 2023`
Record UNII	4T36H88UA7
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

APALUTAMIDE

Official Name

English

APALUTAMIDE [ORANGE BOOK]

Common Name

English

4-(7-(6-CYANO-5-(TRIFLUOROMETHYL)PYRIDIN-3-YL)-8-OXO-6-THIOXO-5,7-DIAZASPIRO(3.4)OCTAN-5-YL)-2-FLUORO-N-METHYLBENZAMIDE

Systematic Name

English

Apalutamide [WHO-DD]

Common Name

English

ERLEADA

Brand Name

English

APALUTAMIDE [MI]

Common Name

English

apalutamide [INN]

Common Name

English

BENZAMIDE, 4-(7-(6-CYANO-5-(TRIFLUOROMETHYL)-3-PYRIDINYL)-8-OXO-6-THIOXO-5,7-DIAZASPIRO(3.4)OCT-5-YL)-2-FLUORO-N-METHYL-

Systematic Name

English

JNJ-56021927

Code

English

APALUTAMIDE [JAN]

Common Name

English

ARN-509

Code

English

Classification Tree Code System Code

WHO-ATC

L02BB05