Enzalutamide

Identification

Summary

Enzalutamide is a second-generation androgen receptor inhibitor used to treat castration-resistant prostate cancer and metastatic castration-sensitive prostate cancer.

Brand Names

Xtandi

Generic Name

Enzalutamide

DrugBank Accession Number

DB08899

Background

Enzalutamide is an androgen receptor (AR) inhibitor for the treatment of castration-resistant prostate cancer (CRPC), both metastatic and non-metastatic.⁸ It is a second-generation antiandrogen agent that the FDA approved on August 31, 2012.^8,7 Although androgen deprivation therapy (ADT) is the first-line treatment of prostate cancer and remission can be achieved, arising resistance is inevitable, becoming castration-resistant prostate cancer.⁷ Until recently, docetaxel is the only treatment available for metastatic CRPC; however, AR inhibitors have been developed for more targeted therapy, although first-generation AR inhibitors like bicalutamide did not substantially increase the survival rate.⁷ Second-generation such as enzalutamide is more efficacious due to a higher affinity to AR and no partial agonist activity compared to bicalutamide.^7,1

Due to a favorable pharmacological profile, a phase 1 study of enzalutamide was initiated in July 2007. Compared to the average time of 10 to 15 years for a drug to go from pre-clinical to clinical studies, enzalutamide was developed relatively rapidly.⁷

Type

Small Molecule

Groups

Approved

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Enzalutamide (DB08899)

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Weight

Average: 464.436
Monoisotopic: 464.093009286

Chemical Formula

C₂₁H₁₆F₄N₄O₂S

Synonyms

• Enzalutamida
• Enzalutamide

External IDs

• MDV 3100
• MDV-3100
• MDV3100

Pharmacology

Indication

Enzalutamide is indicated for the treatment of castration-resistant prostate cancer and metastatic castration-sensitive prostate cancer.⁸

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Associated Conditions

• Castration Resistant Prostate Cancer
• Metastatic Castration Sensitive Prostate Cancer

Contraindications & Blackbox Warnings

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Pharmacodynamics

Enzalutamide is a second-generation antiandrogen that blocks the activity of androgen and androgen receptor (AR) in prostate cancer. AR activity and prostate cancer progression are closely related due to the normal physiology of prostate cells, providing the rationale for androgen deprivation therapy (ADT).⁴ However, resistance will eventually arise after the commencement of ADT in 2-3 years due to the accumulation of mutations, including constitutively active mutation, AR overexpression, and changes in AR splicing variants.^5,1 Enzalutamide was therefore designed to exploit these mutations.³ In vitro experiments in human prostate cancer cell line VCaP showed that enzalutamide can suppress cell growth and induce apoptosis while other antiandrogens like bicalutamide did not.³

Clinical trials on prostate cancer patients indicated that enzalutamide can lead to a decrease in serum PSA for at least 12 weeks, although this response can be short-lived and thus resulting in enzalutamide resistance.^6,3 Patients receiving enzalutamide also had a 37% decreased in the risk of death compared to placebo.²

Mechanism of action

Enzalutamide is a competitive androgen receptor (AR) inhibitor that has a threefold inhibition on the androgen signaling pathway without significant AR agonist activity.^9,1 It inhibits androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with chromosomal DNA to upregulate oncogenes.^1,2 Enzalutamide binds to the AR with 5 to 8-fold greater affinity than first-generation antiandrogens such as bicalutamide and only 2-3 fold reduced affinity than the natural ligand dihydrotestosterone.³ Molecular docking showed that enzalutamide binds to the ligand binding domain of the AR distinctive from that of bicalutamide.¹

Target	Actions	Organism
AAndrogen receptor	inhibitor	Humans

Absorption

The median Tmax is 1 hour (0.5 to 3 hours) following a single 160 mg dose of capsules and 2 hours (0.5 to 6 hours) following a single 160 mg dose of tablets.⁹ Enzalutamide achieves steady-state by Day 28 and its AUC accumulates approximately 8.3-fold relative to a single dose. At steady-state, the mean (%CV) maximum concentration (Cmax) for enzalutamide and N-desmethyl enzalutamide is 16.6 µg/mL (23%) and 12.7 µg/mL (30%), respectively, and the mean (%CV) minimum concentrations (Cmin) are 11.4 µg/mL (26%) and 13.0 µg/mL (30%), respectively.⁹

Volume of distribution

The mean (%CV) volume of distribution after a single oral dose is 110 L (29%).⁹

Protein binding

Enzalutamide is 97% to 98% bound to plasma proteins, primarily albumin. N-desmethyl enzalutamide is 95% bound to plasma proteins.⁹

Metabolism

Enzalutamide is metabolized by CYP2C8 and CYP3A4. CYP2C8 is primarily responsible for the formation of the active metabolite (N-desmethyl enzalutamide). Carboxylesterase 1 metabolizes N-desmethyl enzalutamide and enzalutamide to the inactive carboxylic acid metabolite.⁹

Hover over products below to view reaction partners

• Enzalutamide
  • M6 enzalutamide
    • N-desmethyl enzalutamide
      • Carboxyl metabolite enzalutamide (M1)
  • Carboxyl metabolite enzalutamide (M1)

Route of elimination

Enzalutamide is primarily eliminated by hepatic metabolism. 71% of the dose is recovered in urine (including only trace amounts of enzalutamide and N-desmethyl enzalutamide), and 14% is recovered in feces (0.4% of the dose as unchanged enzalutamide and 1% as N-desmethyl enzalutamide).¹¹

Half-life

The mean terminal half-life (t1/2) for enzalutamide in patients after a single oral dose is 5.8 days (range 2.8 to 10.2 days). Following a single 160 mg oral dose of enzalutamide in healthy volunteers, the mean terminal t1/2 for N-desmethyl enzalutamide is approximately 7.8 to 8.6 days.⁹

Clearance

The mean apparent clearance (CL/F) of enzalutamide after a single dose is 0.56 L/h (0.33 to 1.02 L/h).⁹

Adverse Effects

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Toxicity

In an embryo-fetal developmental toxicity study in mice, enzalutamide caused developmental toxicity when administered at oral doses of 10 or 30 mg/kg/day throughout the period of organogenesis (gestational days 6-15). Findings included embryo-fetal lethality (increased post-implantation loss and resorptions) and decreased anogenital distance at ≥ 10 mg/kg/day, and cleft palate and absent palatine bone at 30 mg/kg/day. Doses of 30 mg/kg/day caused maternal toxicity. The doses tested in mice (1, 10, and 30 mg/kg/day) resulted in systemic exposures (AUC) of approximately 0.04, 0.4, and 1.1 times, respectively, the exposures in patients. Enzalutamide did not cause developmental toxicity in rabbits when administered throughout the period of organogenesis (gestational days 6-18) at dose levels up to 10 mg/kg/day (approximately 0.4 times the exposures in patients based on AUC).⁹

In a pharmacokinetic study in pregnant rats with a single oral 30 mg/kg enzalutamide administration on gestation day 14, enzalutamide and/or its metabolites were present in the fetus at a Cmax that was approximately 0.3 times the concentration found in maternal plasma and occurred 4 hours after administration.⁹

Based on animal studies, XTANDI may impair fertility in males of reproductive potential. Advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 3 months after the last dose of XTANDI.⁹

The most common adverse reactions (≥ 5%) are asthenia/fatigue, back pain, diarrhea, arthralgia, hot flush, peripheral edema, musculoskeletal pain, headache, upper respiratory infection, muscular weakness, dizziness, insomnia, lower respiratory infection, spinal cord compression and cauda equina syndrome, hematuria, paresthesia, anxiety, and hypertension.⁹

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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1,2-Benzodiazepine	The serum concentration of 1,2-Benzodiazepine can be decreased when it is combined with Enzalutamide.
Abacavir	Abacavir may decrease the excretion rate of Enzalutamide which could result in a higher serum level.
Abametapir	The serum concentration of Enzalutamide can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Enzalutamide can be increased when combined with Abatacept.
Abemaciclib	The serum concentration of Abemaciclib can be decreased when it is combined with Enzalutamide.
Abiraterone	The metabolism of Abiraterone can be increased when combined with Enzalutamide.
Abrocitinib	The serum concentration of Abrocitinib can be decreased when it is combined with Enzalutamide.
Acalabrutinib	The serum concentration of Acalabrutinib can be decreased when it is combined with Enzalutamide.
Aceclofenac	Aceclofenac may decrease the excretion rate of Enzalutamide which could result in a higher serum level.
Acemetacin	Acemetacin may decrease the excretion rate of Enzalutamide which could result in a higher serum level.

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Food Interactions

• Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of enzalutamide and may reduce its serum concentration.
• Take with or without food.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Xtandi	Capsule	40 mg	Oral	Astellas Pharma Europe Bv	2016-09-08	Not applicable
Xtandi	Capsule	40 mg	Oral	Astellas Pharma Inc	2013-06-07	Not applicable
Xtandi	Capsule	40 mg/1	Oral	Astellas Pharma US, Inc.	2012-08-31	Not applicable
Xtandi	Tablet	40 mg/1	Oral	Astellas Pharma US, Inc.	2020-08-04	Not applicable
Xtandi	Tablet	80 mg/1	Oral	Astellas Pharma US, Inc.	2020-08-04	Not applicable
Xtandi	Tablet, film coated	40 mg	Oral	Astellas Pharma Europe Bv	2020-12-16	Not applicable
Xtandi	Capsule	40 mg/1	Oral	Astellas Pharma US, Inc.	2012-08-31	Not applicable
Xtandi	Tablet	40 mg/1	Oral	Astellas Pharma US, Inc.	2020-08-04	Not applicable
Xtandi	Tablet, film coated	80 mg	Oral	Astellas Pharma Europe Bv	2020-12-16	Not applicable

Categories

ATC Codes

L02BB04 — Enzalutamide

• L02BB — Anti-androgens
• L02B — HORMONE ANTAGONISTS AND RELATED AGENTS
• L02 — ENDOCRINE THERAPY
• L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Drug Categories

• Amides
• Androgen Receptor Antagonists
• Androgen Receptor Inhibitors
• Antiandrogens
• Antiandrogens, non-steroidal
• Antineoplastic Agents
• Antineoplastic and Immunomodulating Agents
• Benzene Derivatives
• Cytochrome P-450 CYP2B6 Inhibitors
• Cytochrome P-450 CYP2B6 Inhibitors (strength unknown)
• Cytochrome P-450 CYP2C19 Inducers
• Cytochrome P-450 CYP2C19 Inducers (moderate)
• Cytochrome P-450 CYP2C8 Inhibitors
• Cytochrome P-450 CYP2C8 Inhibitors (moderate)
• Cytochrome P-450 CYP2C8 Substrates
• Cytochrome P-450 CYP2C9 Inducers
• Cytochrome P-450 CYP2C9 Inducers (moderate)
• Cytochrome P-450 CYP2C9 Substrates
• Cytochrome P-450 CYP3A Inducers
• Cytochrome P-450 CYP3A Inducers (strong)
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Inducers
• Cytochrome P-450 CYP3A4 Inducers (strong)
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 CYP3A5 Inducers
• Cytochrome P-450 CYP3A5 Inducers (strong)
• Cytochrome P-450 CYP3A5 Substrates
• Cytochrome P-450 Enzyme Inducers
• Cytochrome P-450 Enzyme Inhibitors
• Cytochrome P-450 Substrates
• Drugs that are Mainly Renally Excreted
• Endocrine Therapy
• Hormone Antagonists and Related Agents
• Hydantoins
• Imidazoles
• Imidazolidines
• P-glycoprotein inhibitors
• Thyroxine-binding globulin substrates

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as phenylimidazolidines. These are polycyclic compounds containing an imidazoline substituted by a phenyl group.

Kingdom

Organic compounds

Super Class

Organoheterocyclic compounds

Class

Azolidines

Sub Class

Imidazolidines

Direct Parent

Phenylimidazolidines

Alternative Parents

Trifluoromethylbenzenes / 2-halobenzoic acids and derivatives / Alpha amino acids and derivatives / N-phenylthioureas / Benzamides / Benzoyl derivatives / Benzonitriles / Fluorobenzenes / Aryl fluorides / Imidazolidinones / Vinylogous halides / Thioureas / Secondary carboxylic acid amides / Nitriles / Azacyclic compounds / Carbonyl compounds / Hydrocarbon derivatives / Organic oxides / Organofluorides / Alkyl fluorides / Organopnictogen compounds

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Substituents

2-halobenzoic acid or derivatives / Alkyl fluoride / Alkyl halide / Alpha-amino acid or derivatives / Aromatic heteromonocyclic compound / Aryl fluoride / Aryl halide / Azacycle / Benzamide / Benzenoid / Benzoic acid or derivatives / Benzonitrile / Benzoyl / Carbonitrile / Carbonyl group / Carboxamide group / Carboxylic acid derivative / Fluorobenzene / Halobenzene / Halobenzoic acid or derivatives / Hydrocarbon derivative / Imidazolidinone / Monocyclic benzene moiety / N-phenylthiourea / Nitrile / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organofluoride / Organohalogen compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Organosulfur compound / Phenylimidazolidine / Secondary carboxylic acid amide / Thiourea / Trifluoromethylbenzene / Vinylogous halide

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Molecular Framework

Aromatic heteromonocyclic compounds

External Descriptors

benzamides, nitrile, imidazolidinone, monofluorobenzenes, (trifluoromethyl)benzenes, thiocarbonyl compound (CHEBI:68534)

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

93T0T9GKNU

CAS number

915087-33-1

InChI Key

WXCXUHSOUPDCQV-UHFFFAOYSA-N

InChI

InChI=1S/C21H16F4N4O2S/c1-20(2)18(31)28(12-5-4-11(10-26)15(8-12)21(23,24)25)19(32)29(20)13-6-7-14(16(22)9-13)17(30)27-3/h4-9H,1-3H3,(H,27,30)

IUPAC Name

4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl}-2-fluoro-N-methylbenzamide

SMILES

CNC(=O)C1=C(F)C=C(C=C1)N1C(=S)N(C(=O)C1(C)C)C1=CC=C(C#N)C(=C1)C(F)(F)F

References

General References

1. Schalken J, Fitzpatrick JM: Enzalutamide: targeting the androgen signalling pathway in metastatic castration-resistant prostate cancer. BJU Int. 2016 Feb;117(2):215-25. doi: 10.1111/bju.13123. Epub 2015 Jun 6. [Article]
2. Saad F: Evidence for the efficacy of enzalutamide in postchemotherapy metastatic castrate-resistant prostate cancer. Ther Adv Urol. 2013 Aug;5(4):201-10. doi: 10.1177/1756287213490054. [Article]
3. Tran C, Ouk S, Clegg NJ, Chen Y, Watson PA, Arora V, Wongvipat J, Smith-Jones PM, Yoo D, Kwon A, Wasielewska T, Welsbie D, Chen CD, Higano CS, Beer TM, Hung DT, Scher HI, Jung ME, Sawyers CL: Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90. doi: 10.1126/science.1168175. Epub 2009 Apr 9. [Article]
4. Heinlein CA, Chang C: Androgen receptor in prostate cancer. Endocr Rev. 2004 Apr;25(2):276-308. doi: 10.1210/er.2002-0032. [Article]
5. Fujita K, Nonomura N: Role of Androgen Receptor in Prostate Cancer: A Review. World J Mens Health. 2019 Sep;37(3):288-295. doi: 10.5534/wjmh.180040. Epub 2018 Sep 10. [Article]
6. Tan MH, Li J, Xu HE, Melcher K, Yong EL: Androgen receptor: structure, role in prostate cancer and drug discovery. Acta Pharmacol Sin. 2015 Jan;36(1):3-23. doi: 10.1038/aps.2014.18. Epub 2014 Jun 9. [Article]
7. Menon MP, Higano CS: Enzalutamide, a second generation androgen receptor antagonist: development and clinical applications in prostate cancer. Curr Oncol Rep. 2013 Apr;15(2):69-75. doi: 10.1007/s11912-013-0293-9. [Article]
8. FDA Approved Drug Products: Xtandi (enzalutamide) capsules/tablets for oral use [Link]
9. FDA Approved Drug Products: Xtandi (enzalutamide) capsules/tablets for oral use 2022 [Link]
10. Health Canada Approved Drug Products: Xtandi (enzalutamide) capsules/tablets for oral use 2022 [Link]
11. Enzalutamide FDA label [Link]

External Links

Human Metabolome Database

HMDB0251831

KEGG Drug

D10218

PubChem Compound

15951529

PubChem Substance

175427141

ChemSpider

13093347

BindingDB

50425732

RxNav

1307298

ChEBI

68534

ChEMBL

CHEMBL1082407

ZINC

ZINC000034806477

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

Wikipedia

Enzalutamide

FDA label

Download (393 KB)

MSDS

Download (89.7 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Metastatic Castration Resistant Prostate Cancer (CRPC)	1
4	Completed	Treatment	Metastatic Castration Resistant Prostate Cancer (CRPC)	2
4	Completed	Treatment	Prostate Cancer	2
4	Completed	Treatment	Refractory, metastatic hormone-refractory Prostate cancer	1
4	Recruiting	Supportive Care	Castration Resistant Prostatic Cancer / Hormone Refractory Prostate Cancer / Recurrent Prostate Carcinoma / Refractory, metastatic hormone-refractory Prostate cancer / Stage IV Prostate Cancer	1
4	Recruiting	Treatment	Castration Resistant Prostatic Neoplasms	1
4	Recruiting	Treatment	Metastatic Castration Resistant Prostate Cancer (CRPC)	1
4	Terminated	Treatment	Metastatic Castration Resistant Prostate Cancer (CRPC)	1
3	Active Not Recruiting	Treatment	Adenocarcinoma of the Prostate / Hormone Resistant Prostate Cancer / Prostate Cancer - Recurrent / Stage IV Prostate Cancer	1
3	Active Not Recruiting	Treatment	Castration Resistant Prostatic Neoplasms	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Capsule	Oral
Capsule	Oral	40 mg/1
Tablet	Oral	40 mg/1
Tablet	Oral	80 mg/1
Tablet, film coated	Oral	40 MG
Tablet, film coated	Oral	80 MG
Capsule, liquid filled	Oral	40 mg
Capsule	Oral	40 mg
Capsule, liquid filled	Oral	40.0 mg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US8183274	No	2012-05-22	2026-05-15
US9126941	No	2015-09-08	2026-05-15
US7709517	No	2010-05-04	2027-08-13

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	201 ºC	L43242
water solubility	Insoluble	FDA label
logP	3.0	L43242

Predicted Properties

Property	Value	Source
Water Solubility	0.00136 mg/mL	ALOGPS
logP	3.75	ALOGPS
logP	4.16	Chemaxon
logS	-5.5	ALOGPS
pKa (Strongest Acidic)	13.05	Chemaxon
pKa (Strongest Basic)	-1.6	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	3	Chemaxon
Hydrogen Donor Count	1	Chemaxon
Polar Surface Area	76.44 Å2	Chemaxon
Rotatable Bond Count	4	Chemaxon
Refractivity	113.48 m3·mol-1	Chemaxon
Polarizability	42.69 Å3	Chemaxon
Number of Rings	3	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9356
Blood Brain Barrier	+	0.8514
Caco-2 permeable	+	0.5219
P-glycoprotein substrate	Non-substrate	0.7609
P-glycoprotein inhibitor I	Inhibitor	0.6464
P-glycoprotein inhibitor II	Inhibitor	0.5693
Renal organic cation transporter	Non-inhibitor	0.899
CYP450 2C9 substrate	Non-substrate	0.7447
CYP450 2D6 substrate	Non-substrate	0.8061
CYP450 3A4 substrate	Substrate	0.5589
CYP450 1A2 substrate	Non-inhibitor	0.5613
CYP450 2C9 inhibitor	Inhibitor	0.7126
CYP450 2D6 inhibitor	Non-inhibitor	0.9148
CYP450 2C19 inhibitor	Inhibitor	0.6882
CYP450 3A4 inhibitor	Inhibitor	0.6184
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.6711
Ames test	Non AMES toxic	0.683
Carcinogenicity	Non-carcinogens	0.7232
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.4319 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9911
hERG inhibition (predictor II)	Inhibitor	0.7079

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
MS/MS Spectrum - , positive	LC-MS/MS	splash10-014i-0321900000-b1c610c4a717fdea030e

Targets

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Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	>100000	N/A	N/A	A29488

Details

Binding Properties1. Androgen receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Zinc ion binding

Specific Function

Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...

Gene Name

AR

Uniprot ID

P10275

Uniprot Name

Androgen receptor

Molecular Weight

98987.9 Da

References

1. FDA Approved Drug Products: Xtandi (enzalutamide) capsules/tablets for oral use 2022 [Link]

×

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Drug created at June 05, 2013 05:12 / Updated at December 01, 2022 23:18