Apalutamide

Highest phase reached
Approved
www.ebi.ac.uk
Drug type
Small molecule
www.ebi.ac.uk
First approval year
2018
www.ebi.ac.uk

First approval year
2018
www.ebi.ac.uk
Listing at source
Listed
Highest phase reached
Approved
www.ebi.ac.uk

Drug type
Small molecule
www.ebi.ac.uk
Drug name
Apalutamide
www.ebi.ac.uk
Molecular weight
477.44
www.ebi.ac.uk
Structure (SMILES)
CNC(=O)c1ccc(N2C(=S)N(c3cnc(C#N)c(C(F)(F)F)c3)C(=O)C23CCC3)cc1F
www.ebi.ac.uk

  • erleada
  • Erleada

  • apalutamida
  • Apalutamida
  • apalutamide
  • Apalutamide
  • Apalutamide (Erleada™) 60 mg or 240 mg tablets
  • Apalutamide [INN]
  • Apalutamide [JAN]
  • Apalutamide [MI]
  • Apalutamide [ORANGE BOOK]
  • Apalutamide [WHO-DD]
  • Apalutamide 240 mg
  • apalutamide inn
  • apalutamide jan
  • apalutamide mi
  • Apalutamide Oral Tablet
  • apalutamide orange book
  • apalutamide who dd
  • arn 509
  • Arn-509
  • ARN-509
  • ARN-509 (Phase 1)
  • ARN-509 (Phase 2)
  • jnj 56021927
  • JNJ 56021927
  • JNJ-56021927

And 2 more, listed on the interactive page.

ATC classification codes
  • L02BB05
Sources for recorded values
www.ebi.ac.uk
CAS registry numbers
  • 956104-40-8
ChEMBL ID
CHEMBL3183409
www.ebi.ac.uk
InChIKey
HJBWBFZLDZWPHF-UHFFFAOYSA-N
www.ebi.ac.uk
PubChem compound IDs
  • 24872560
RxNorm IDs (RxCUI)
  • 1999574
FDA ingredient codes (UNII)
  • 4T36H88UA7

Applicant
JANSSEN BIOTECH
Approval date
14 Feb 2018
Application number
NDA210951

Status
Authorised
Status date
14 Jan 2019
Authorisation date
14 Jan 2019
Approved indications
Erleada is indicated: in adult men for the treatment of non metastatic castration resistant prostate cancer (nmCRPC) who are at high risk of developing metastatic disease. in adult men for the treatment of metastatic hormone-sensitive prostate cancer (mHSPC) in combination with androgen deprivation therapy (ADT).
Product number
EMEA/H/C/004452
Authorisation holder
Janssen-Cilag International NV
Priority medicines scheme
No
Generic
No
Biosimilar
No
Generic medicines
0
Biosimilar medicines
0
Advanced therapy
No
Conditional approval
No
Additional monitoring
No
Accelerated assessment
No
Exceptional circumstances
No

Therapeutic areas

  • Prostatic Neoplasms
European medicines record
www.ema.europa.eu

Patents
14
Designations
2
Earliest recorded loss of exclusivity
14 Jan 2041
First in class
No
Fast track
Yes
Breakthrough designation
No
Orphan designation
No
Priority review
Yes
Orphan exclusivity
No
Accelerated approval
No
Availability
Prescription only

Pharmacology name
apalutamide
Type
Synthetic organic
Drug name stem
-lutamide
Approval recorded by Guide to Pharmacology
Yes

Administration routes

  • Oral

  • Action
    Antagonist
    Action type
    Antagonist
    Target
    Androgen receptor
    Gene symbol
    AR
    Protein identifier
    P10275
    Median affinity
    6.7
    Affinity units
    pIC50
    Primary target
    Yes
  • Mechanism
    Androgen Receptor antagonist
    Action type
    Antagonist
    Target
    Androgen receptor
    Protein identifier
    P10275

Open Targets mechanisms

  • Mechanism
    Androgen Receptor antagonist
    Action type
    Antagonist
    Target
    Androgen receptor

DrugCentral mechanisms

  • Action type
    Inhibitor
    Gene symbol
    AR
    Protein identifier
    P10275
    Organism
    Homo sapiens
    Target development level
    Clinical

  • Condition
    Prostatic Neoplasms
    Highest recorded phase
    4
    Condition identifier
    EFO:0000196
    Subject identifier
    D011471
  • Condition
    Neoplasms
    Highest recorded phase
    4
    Condition identifier
    EFO:0000616
    Subject identifier
    D009369
  • Condition
    Prostatic Neoplasms
    Highest recorded phase
    4
    Condition identifier
    EFO:0000673
    Subject identifier
    D011471
  • Condition
    Liver Diseases
    Highest recorded phase
    1
    Condition identifier
    EFO:0001421
    Subject identifier
    D008107
  • Condition
    Prostatic Neoplasms
    Highest recorded phase
    4
    Condition identifier
    EFO:0001663
    Subject identifier
    D011471
  • Condition
    Prostatic Neoplasms, Castration-Resistant
    Highest recorded phase
    4
    Condition identifier
    EFO:0001663
    Subject identifier
    D064129
  • Condition
    Salivary Gland Neoplasms
    Highest recorded phase
    2
    Condition identifier
    EFO:0003826
    Subject identifier
    D012468
  • Condition
    Neoplasms
    Highest recorded phase
    4
    Condition identifier
    MONDO:0004992
    Subject identifier
    D009369
  • Condition
    Prostatic Neoplasms
    Highest recorded phase
    4
    Condition identifier
    MONDO:0008315
    Subject identifier
    D011471
  • Condition
    Prostatic Neoplasms, Castration-Resistant
    Highest recorded phase
    4
    Condition identifier
    MONDO:0008315
    Subject identifier
    D064129

  • Condition identifier
    EFO_0000196
    Highest recorded phase
    2
  • Condition identifier
    EFO_0000616
  • Condition identifier
    EFO_0000673
    Highest recorded phase
    3
  • Condition identifier
    EFO_0001421
    Highest recorded phase
    1
  • Condition identifier
    EFO_0001663
  • Condition identifier
    EFO_0003826
    Highest recorded phase
    2
  • Condition identifier
    EFO_0004920
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0000521
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0004956
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0004992
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0005070
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0005082
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005159
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0008315
  • Condition identifier
    MONDO_0008315
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0015667
  • Condition identifier
    MONDO_0015667
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0021259
    Highest recorded phase
    4

  • Event
    blood thyroid stimulating hormone increased
    Reports
    16
    Reporting signal score
    33.2639
  • Event
    decreased appetite
    Reports
    66
    Reporting signal score
    40.9002
  • Event
    dermatitis exfoliative generalised
    Reports
    11
    Reporting signal score
    24.452
  • Event
    disease progression
    Reports
    49
    Reporting signal score
    36.4677
  • Event
    fatigue
    Reports
    164
    Reporting signal score
    60.759
  • Event
    headache
    Reports
    13
    Reporting signal score
    20.9081
  • Event
    hot flush
    Reports
    71
    Reporting signal score
    127.469
  • Event
    prostate cancer
    Reports
    15
    Reporting signal score
    19.1271
  • Event
    prostatic specific antigen decreased
    Reports
    5
    Reporting signal score
    22.3018
  • Event
    prostatic specific antigen increased
    Reports
    47
    Reporting signal score
    135.867
  • Event
    pruritus
    Reports
    65
    Reporting signal score
    21.8574
  • Event
    rash
    Reports
    282
    Reporting signal score
    313.942
  • Event
    vomiting
    Reports
    10
    Reporting signal score
    21.3464

And 61 more, listed on the interactive page.

Dose
240mg
Route
Oral
How often
Once daily

  • Can be taken with or without food
  • Swallow tablets whole

Hydrogen bond acceptors
5
Hydrogen bond donors
1
Polar surface area
89.33
Calculated partition coefficient (ALogP)
3.53
Calculated partition coefficient (XLogP)
3
Prodrug
No
Chirality
Achiral
Inorganic
No
Rule-of-five violations
0
Rotatable bonds
3
Heavy atoms
33
Molecular formula
C21H15F4N5O2S
Monoisotopic mass
477.08825856
Natural product
No

  • 59676-600
  • 59676-604

Recorded assays
470
Active assays
102

  • Confirmatory
  • Other
  • Screening

Related records

Trials (147)

Approved for (6)

In development for (2)

Other linked conditions (1)

Targets (1)