> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/tucatinib-79f88fe2-698e-4d56-aaf9-f0c4927094ba
> Record changed: 2026-10-13

# Tucatinib

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

First approval year

2020

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

## Development status

**First approval year**

2020

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

**Drug name**

Tucatinib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

**Molecular weight**

480.53

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

**Structure (SMILES)**

Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

### Brand names (2)

- tukysa
- Tukysa

### Other names (26)

- 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.

## Identifiers

**ATC classification codes**

- L01EH03

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

**CAS registry numbers**

- 937263-43-9

**ChEMBL ID**

CHEMBL3989868

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

**InChIKey**

SDEAXTCZPQIFQM-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3989868)

**PubChem compound IDs**

- 51039094

**RxNorm IDs (RxCUI)**

- 2361285

**FDA ingredient codes (UNII)**

- 234248D0HH

## Regulatory information

### United States

**Applicant**

SEAGEN

**Approval date**

17 Apr 2020

**Application number**

NDA213411

### European Union

**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

Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/tukysa)

### Other regulatory facts

**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

### Drug classification

**Pharmacology name**

tucatinib

**Type**

Synthetic organic

**Drug name stem**

\-tinib

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (4)

- **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

### DrugCentral mechanisms (3)

- **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

### Investigated indications (17)

- **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

### Open Targets indications (31)

- **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.

### Reported adverse events (60)

- **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.

### Trial references (34)

- NCT00650572  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00650572)
- NCT02892123  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02892123)
- NCT04632992  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04632992)
- NCT01042379  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01042379)
- NCT01921335  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01921335)
- NCT01983501  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01983501)
- NCT02025192  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02025192)
- NCT02614794  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02614794)
- NCT03054363  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03054363)
- NCT03846583  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03846583)
- NCT04538742  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04538742)
- NCT04721977  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04721977)
- NCT04789096  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04789096)
- NCT04896320  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04896320)
- NCT05041842  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05041842)
- NCT05227131  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05227131)
- NCT05230810  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05230810)
- NCT05458674  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05458674)
- NCT05748834  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05748834)
- NCT05892068  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05892068)
- NCT06162559  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06162559)
- NCT03722823  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03722823)
- NCT03799094  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03799094)
- NCT06067776  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06067776)
- NCT04006847  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04006847)

And 9 more, listed on the interactive page.

## Dosing

**Dose**

300 mg

**Route**

Oral

**How often**

Twice daily

### Conditions of use (2)

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

## Chemical properties

**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

## National Drug Codes

- 51144-001
- 51144-002

## Evidence counts

**Recorded assays**

593

**Active assays**

45

### Active assay types (2)

- Confirmatory
- Screening

## Pharmacologic actions

- Antineoplastic Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000970.html)
- Protein Kinase Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D047428.html)

## 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)

- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md)
- Breast carcinoma
- [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md)
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md)
- [Colorectal carcinoma](https://trialight.com/data/condition/colorectal-carcinoma-51401c02-7884-5c5c-bb91-90106e7d0d4a.md)
- [Colorectal neoplasm](https://trialight.com/data/condition/colorectal-neoplasm-31f0a633-3abe-5df4-9d3a-9292c6541f1d.md)
- [HER2 positive breast carcinoma](https://trialight.com/data/condition/her2-positive-breast-carcinoma-eb8493ec-908e-5435-bf56-0d20c0c9bb88.md)
- Neoplasm

### In development for (8)

- Angiosarcoma Phase 2
- Chronic myeloid leukemia Phase 1
- Colon carcinoma Phase 2
- [Gastric cancer](https://trialight.com/data/condition/gastric-cancer-3c1e2785-2672-5b3e-afce-9335f684c159.md) Phase 2
- [Hepatocellular carcinoma](https://trialight.com/data/condition/hepatocellular-carcinoma-fc1014ac-5a3c-551d-98ea-95306009e299.md) Phase 1
- [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1
- [Lung cancer](https://trialight.com/data/condition/lung-cancer-c4ca1fe0-9b3d-5957-a668-2d6cf26bd16a.md) Phase 1
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 1

### Other linked conditions (1)

- [Gastric adenocarcinoma](https://trialight.com/data/condition/gastric-adenocarcinoma-6bb74a55-7ba6-53e3-a113-22296a84d6ae.md)

### Targets (1)

- [ERBB2](https://trialight.com/data/target/erbb2-900ec94b-8cc2-5864-a53d-4b5ed23c71f5.md) Receptor protein-tyrosine kinase erbB-2 inhibitor

---

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