Tucatinib

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

2020

www.ebi.ac.uk

First approval year: 2020
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: Tucatinib
www.ebi.ac.uk

Molecular weight: 480.53
www.ebi.ac.uk

Structure (SMILES): Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1
www.ebi.ac.uk

tukysa
Tukysa

arry 380
ARRY-380
cinrebafusp alfa prs 343 in combination with tucatinib
irbinitinib
Irbinitinib
mk 7119
MK-7119
ont 380
Ont-380
ONT-380
tucatinib
Tucatinib
Tucatinib (ONT-380)
tucatinib [INN]
TUCATINIB [MI]
TUCATINIB [ORANGE BOOK]
TUCATINIB [USAN]
Tucatinib [WHO-DD]
Tucatinib 150 MG
tucatinib inn
tucatinib mi
Tucatinib Oral Tablet
tucatinib orange book
tucatinib usan
tucatinib who dd

And 1 more, listed on the interactive page.

ATC classification codes

L01EH03

Sources for recorded values

www.ebi.ac.uk

CAS registry numbers

937263-43-9

ChEMBL ID: CHEMBL3989868
www.ebi.ac.uk

InChIKey: SDEAXTCZPQIFQM-UHFFFAOYSA-N
www.ebi.ac.uk

PubChem compound IDs

51039094

RxNorm IDs (RxCUI)

2361285

FDA ingredient codes (UNII)

234248D0HH

Applicant: SEAGEN
Approval date: 17 Apr 2020
Application number: NDA213411

Status: Authorised
Status date: 11 Feb 2021
Authorisation date: 11 Feb 2021
Approved indications: Tukysa is indicated in combination with trastuzumab and capecitabine for the treatment of adult patients with HER2?positive locally advanced or metastatic breast cancer who have received at least 2 prior anti-HER2 treatment regimens.
Product number: EMEA/H/C/005263
Authorisation holder: Pfizer Europe MA EEIG
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

Breast Neoplasms
Neoplasm Metastasis

European medicines record

www.ema.europa.eu

Patents: 7
Designations: 6
Earliest recorded loss of exclusivity: 27 Apr 2038
First in class: No
Fast track: Yes
Breakthrough designation: Yes
Orphan designation: No
Priority review: Yes
Orphan exclusivity: No
Accelerated approval: No
Availability: Prescription only

Pharmacology name: tucatinib
Type: Synthetic organic
Drug name stem: -tinib
Approval recorded by Guide to Pharmacology: Yes

Administration routes

Oral

Action
Inhibition
Action type
Inhibitor
Target
epidermal growth factor receptor
Gene symbol
EGFR
Protein identifier
P00533
Median affinity
6.35
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
erb-b2 receptor tyrosine kinase 2
Gene symbol
ERBB2
Protein identifier
P04626
Median affinity
8.16
Affinity units
pIC50
Primary target
Yes
Action
Inhibition
Action type
Inhibitor
Target
erb-b2 receptor tyrosine kinase 4
Gene symbol
ERBB4
Protein identifier
Q15303
Median affinity
6.51
Affinity units
pIC50
Mechanism
Receptor protein-tyrosine kinase erbB-2 inhibitor
Action type
Inhibitor
Target
Receptor tyrosine-protein kinase erbB-2
Protein identifier
P04626

Open Targets mechanisms

Mechanism
Receptor protein-tyrosine kinase erbB-2 inhibitor
Action type
Inhibitor
Target
Receptor tyrosine-protein kinase erbB-2

Action type
Inhibitor
Gene symbol
EGFR
Protein identifier
P00533
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
ERBB2|ERBB3
Protein identifier
P04626|P21860
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
ERBB4
Protein identifier
Q15303
Organism
Homo sapiens
Target development level
Clinical

Condition
Carcinoma, Hepatocellular
Highest recorded phase
1
Condition identifier
EFO:0000182
Subject identifier
D006528
Condition
Breast Neoplasms
Highest recorded phase
4
Condition identifier
EFO:0000305
Subject identifier
D001943
Condition
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Highest recorded phase
1
Condition identifier
EFO:0000339
Subject identifier
D015464
Condition
Neoplasms
Highest recorded phase
4
Condition identifier
EFO:0000616
Subject identifier
D009369
Condition
Liver Diseases
Highest recorded phase
1
Condition identifier
EFO:0001421
Subject identifier
D008107
Condition
Carcinoma, Non-Small-Cell Lung
Highest recorded phase
1
Condition identifier
EFO:0003060
Subject identifier
D002289
Condition
Breast Neoplasms
Highest recorded phase
4
Condition identifier
EFO:0003869
Subject identifier
D001943
Condition
Hemangiosarcoma
Highest recorded phase
2
Condition identifier
EFO:0003968
Subject identifier
D006394
Condition
Colorectal Neoplasms
Highest recorded phase
4
Condition identifier
EFO:0004142
Subject identifier
D015179
Condition
Neoplasm Metastasis
Highest recorded phase
4
Condition identifier
EFO:0009708
Subject identifier
D009362
Condition
Breast Neoplasms
Highest recorded phase
4
Condition identifier
EFO:1000294
Subject identifier
D001943
Condition
Colonic Neoplasms
Highest recorded phase
2
Condition identifier
EFO:1001950
Subject identifier
D003110
Condition
Colorectal Neoplasms
Highest recorded phase
4
Condition identifier
EFO:1001951
Subject identifier
D015179
Condition
Stomach Neoplasms
Highest recorded phase
2
Condition identifier
MONDO:0001056
Subject identifier
D013274
Condition
Neoplasms
Highest recorded phase
4
Condition identifier
MONDO:0004992
Subject identifier
D009369
Condition
Breast Neoplasms
Highest recorded phase
4
Condition identifier
MONDO:0007254
Subject identifier
D001943
Condition
Lung Neoplasms
Highest recorded phase
1
Condition identifier
MONDO:0008903
Subject identifier
D008175

Condition identifier
EFO_0000339
Condition identifier
EFO_0000503
Condition identifier
EFO_0000616
Condition identifier
EFO_0001421
Highest recorded phase
1
Condition identifier
EFO_0003869
Condition identifier
EFO_0009708
Condition identifier
EFO_0009708
Highest recorded phase
4
Condition identifier
EFO_1000294
Condition identifier
EFO_1001012
Highest recorded phase
2
Condition identifier
EFO_1001951
Condition identifier
MONDO_0001056
Highest recorded phase
2
Condition identifier
MONDO_0002169
Highest recorded phase
2
Condition identifier
MONDO_0002715
Highest recorded phase
2
Condition identifier
MONDO_0002974
Highest recorded phase
2
Condition identifier
MONDO_0003060
Highest recorded phase
2
Condition identifier
MONDO_0003219
Highest recorded phase
2
Condition identifier
MONDO_0004989
Highest recorded phase
4
Condition identifier
MONDO_0004992
Highest recorded phase
2
Condition identifier
MONDO_0005036
Highest recorded phase
2
Condition identifier
MONDO_0005061
Highest recorded phase
1
Condition identifier
MONDO_0005070
Highest recorded phase
4
Condition identifier
MONDO_0005233
Highest recorded phase
3
Condition identifier
MONDO_0005575
Highest recorded phase
3
Condition identifier
MONDO_0006244
Highest recorded phase
4
Condition identifier
MONDO_0007254

And 6 more, listed on the interactive page.

Event
abdominal discomfort
Reports
27
Reporting signal score
16.5498
Event
abdominal distension
Reports
26
Reporting signal score
23.9716
Event
abdominal pain upper
Reports
34
Reporting signal score
19.2683
Event
asthenia
Reports
65
Reporting signal score
31.0201
Event
biopsy
Reports
5
Reporting signal score
17.8276
Event
blister
Reports
16
Reporting signal score
13.9415
Event
blood bilirubin increased
Reports
28
Reporting signal score
43.0133
Event
blood lactate dehydrogenase abnormal
Reports
5
Reporting signal score
20.4751
Event
blood potassium decreased
Reports
16
Reporting signal score
20.1437
Event
botryomycosis
Reports
3
Reporting signal score
17.0148
Event
brain neoplasm
Reports
13
Reporting signal score
34.3018
Event
brain oedema
Reports
11
Reporting signal score
21.5997
Event
brain operation
Reports
6
Reporting signal score
20.9153
Event
breast cancer recurrent
Reports
7
Reporting signal score
17.5509
Event
cell death
Reports
6
Reporting signal score
14.5502
Event
constipation
Reports
64
Reporting signal score
59.613
Event
decreased appetite
Reports
97
Reporting signal score
128.608
Event
dehydration
Reports
43
Reporting signal score
33.6428
Event
diarrhoea
Reports
449
Reporting signal score
800.405
Event
disease progression
Reports
74
Reporting signal score
110.378
Event
drug hypersensitivity
Reports
1
Reporting signal score
14.1719
Event
dry skin
Reports
32
Reporting signal score
48.1867
Event
dyspepsia
Reports
27
Reporting signal score
27.9858
Event
erythema
Reports
39
Reporting signal score
24.3622
Event
faeces soft
Reports
13
Reporting signal score
37.962

And 35 more, listed on the interactive page.

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clinicaltrials.gov
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NCT04721977
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NCT05748834
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NCT06067776
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NCT04006847
clinicaltrials.gov

And 9 more, listed on the interactive page.

Dose: 300 mg
Route: Oral
How often: Twice daily

Swallow tablets whole, do not chew, crush, or split
Take with or without food

Hydrogen bond acceptors: 10
Hydrogen bond donors: 2
Polar surface area: 110.85
Calculated partition coefficient (ALogP): 5.09
Calculated partition coefficient (XLogP): 4
Prodrug: No
Chirality: Achiral
Inorganic: No
Rule-of-five violations: 1
Rotatable bonds: 5
Heavy atoms: 36
Molecular formula: C26H24N8O2
Monoisotopic mass: 480.20222204
Natural product: Yes

51144-001
51144-002

Recorded assays: 593
Active assays: 45

Confirmatory
Screening

Antineoplastic Agents
id.nlm.nih.gov
Protein Kinase Inhibitors
id.nlm.nih.gov

Related records

Trials (68)

A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib
A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib on Metformin
A Phase 1b/2 Study of T-DXd Combinations in HER2-positive Metastatic Breast Cancer
A Phase II Study of Tucatinib and Ado-trastuzumab Emtansine (T-DM1) in Patients With HER2-positive Metastatic Solid Tumors and Metastases to Brain (TUCATEMEB)
A Safety and Activity Study of SBT6050 in Combination With Other HER2-directed Therapies for HER2-positive Cancers
A Safety Study of Tucatinib in Healthy and Hepatically-Impaired Subjects
A Safety, Tolerability, and Pharmacokinetic Study of Tucatinib in Healthy Japanese and Caucasian Subjects
A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response
A Study of ARRY-380 in Patients With Advanced HER2+ Cancer
A Study of Disitamab Vedotin With Other Anticancer Drugs in Solid Tumors
A Study of the Absorption, Metabolism, and Excretion of Tucatinib in Healthy Participants
A Study of Tucatinib (MK-7119) in Combination With Trastuzumab and Capecitabine in Participants With Previously Treated Locally Advanced Unresectable or Metastatic Human Epidermal Growth Factor Receptor 2 Positive (HER2+) Breast Carcinoma (MK-7119-001)
A Study of Tucatinib (ONT-380) Combined With Ado-trastuzumab Emtansine (T-DM1) in Patients With HER2+ Breast Cancer
A Study of Tucatinib (ONT-380) Combined With Capecitabine and/or Trastuzumab in Patients With HER2+ Metastatic Breast Cancer
A Study of Tucatinib and Trastuzumab in People With Rectal Cancer
A Study of Tucatinib Given Before Surgery to People With HER2+ Cancers That Have Spread to the Brain
A Study of Tucatinib or Placebo With Trastuzumab and Pertuzumab for Metastatic HER2+ Breast Cancer
A Study of Tucatinib Plus Trastuzumab Deruxtecan in HER2+ Breast Cancer
A Study of Tucatinib vs. Placebo in Combination With Ado-trastuzumab Emtansine (T-DM1) for Patients With Advanced or Metastatic HER2+ Breast Cancer
A Study of Tucatinib vs. Placebo in Combination With Capecitabine & Trastuzumab in Patients With Advanced HER2+ Breast Cancer

Approved for (8)

In development for (8)

Angiosarcoma Phase 2
Chronic myeloid leukemia Phase 1
Colon carcinoma Phase 2
Gastric cancer Phase 2
Hepatocellular carcinoma Phase 1
Liver disorder Phase 1
Lung cancer Phase 1
Non-small cell lung carcinoma Phase 1

Targets (1)

ERBB2 Receptor protein-tyrosine kinase erbB-2 inhibitor

Tucatinib

Development status

Names and chemistry

Brand names (2)

Other names (26)

Identifiers

Regulatory information

United States

European Union

Therapeutic areas

Other regulatory facts

Pharmacology

Drug classification

Administration routes

Mechanisms of action (4)

Open Targets mechanisms

DrugCentral mechanisms (3)

Investigated indications (17)

Open Targets indications (31)

Reported adverse events (60)

Trial references (34)

Dosing

Conditions of use (2)

Chemical properties

National Drug Codes

Evidence counts

Active assay types (2)

Pharmacologic actions

Related records

Trials (68)

Approved for (8)

In development for (8)

Other linked conditions (1)

Targets (1)