Apalutamide

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Apalutamide is an ofp drug catalogued in DrugCentral. It was first approved by the FDA in 2018. DrugCentral lists 2 molecular targets, including AR and Ar. Recorded indications include Castration-resistant prostate cancer, Malignant tumor of prostate and Metastasis from malignant tumor of prostate.

• Approval status: ofp (first approved 2018 by the FDA).
• Molecular targets: AR and Ar (2 listed in DrugCentral).
• Indications: Castration-resistant prostate cancer, Malignant tumor of prostate and Metastasis from malignant tumor of prostate.
• ATC code: L02BB05 (Anti-androgens).
• Molecular formula: C21H15F4N5O2S; molecular weight 477.44 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Castration-resistant prostate cancer
• Malignant tumor of prostate
• Metastasis from malignant tumor of prostate

Contraindications (1)

• Pregnancy, function

Mechanism & targets

Molecular targets (2)

Target	Gene	Action	Activity
Androgen receptor	AR	inhibitor	IC50 7.80
Androgen receptor	Ar	antagonist	Ki 7.03

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2019-03-26	PMDA	—	Janssen Pharmaceutical K.K.
2019-01-14	EMA	—	JANSSEN-CILAG INTERNATIONAL N.V.
2018-02-14	FDA	—	JANSSEN BIOTECH

ATC classification

ATC code	Therapeutic hierarchy
L02BB05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONE ANTAGONISTS AND RELATED AGENTS › Anti-androgens

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Rash	1162.5
Hot flush	624.5
Death	509.7
Prostatic specific antigen increased	493.4
Fatigue	153.6
Dermatitis exfoliative generalised	131.3
Hospitalisation	108.7
Interstitial lung disease	91.7
Hypothyroidism	91.0
Drug reaction with eosinophilia and systemic symptoms	87.8
Prostate cancer metastatic	85.7
Blood thyroid stimulating hormone increased	84.0

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Apalutamide is on its molecule page.

• Molecular formula: C₂₁H₁₅F₄N₅O₂S
• Molecular weight: 477.44 g/mol
• CAS number: 956104-40-8
• InChIKey: HJBWBFZLDZWPHF-UHFFFAOYSA-N
• PubChem CID: 24872560

CNC(=O)C1=CC=C(C=C1F)N1C(=S)N(C(=O)C11CCC1)C1=CC(=C(N=C1)C#N)C(F)(F)F

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Apalutamide used for?

DrugCentral lists the following indications for Apalutamide: Castration-resistant prostate cancer, Malignant tumor of prostate and Metastasis from malignant tumor of prostate.

How does Apalutamide work?

Its molecular targets in DrugCentral include AR (inhibitor) and Ar (antagonist).

When was Apalutamide first approved?

Apalutamide was first approved by the FDA in 2018.

What is the chemical formula of Apalutamide?

Apalutamide has the molecular formula C21H15F4N5O2S and a molecular weight of 477.44 g/mol.

Sources

• DrugCentral drug card 5278 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3183409 — compound record and bioactivity
• PubChem CID 24872560 — chemical identifiers
• DrugBank DB11901 — drug record
• FDA UNII 4T36H88UA7 — substance identity
• DailyMed: FDA labels for Apalutamide — current prescribing information (label search)
• UniProt P10275 (AR) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.