> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/pyrotinib-a208031f-d802-4094-a71b-838e40d445c1
> Record changed: 2026-11-04

# Pyrotinib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

**Drug name**

Pyrotinib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

**Molecular weight**

583.09

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

**Structure (SMILES)**

CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/\[C@H\]1CCCN1C

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

### Other names (43)

- albumin bound paclitaxel trastuzumab pyrotinib
- capecitabine and pyrotinib
- dalpiciclib pyrotinib
- gq1001 pyrotinib
- her2 pyrotinib pertuzumab trastuzumab
- inetetamab pyrotinib nab paclitaxel
- palbociclib and exemestane plus trastuzumab and pyrotinib
- palbociclib trastuzumab pyrotinib and fulvestrant
- pyrotinib
- Pyrotinib
- Pyrotinib \[WHO-DD\]
- pyrotinib 240mg
- Pyrotinib 240mg
- pyrotinib 320mg
- Pyrotinib 320mg
- pyrotinib 400mg
- Pyrotinib 400mg
- pyrotinib and trastuzumab
- pyrotinib capecitabine bevacizumab
- pyrotinib maleate dalpiciclib trastuzumab letrozole
- pyrotinib maleate plus letrozole
- pyrotinib maleate shr6390 letrozole
- pyrotinib maleate tablets
- Pyrotinib Maleate Tablets
- pyrotinib maleate tablets nab paclitaxel

And 18 more, listed on the interactive page.

## Identifiers

**CAS registry numbers**

- 1269662-73-8

**ChEMBL ID**

CHEMBL3647420

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

**InChIKey**

SADXACCFNXBCFY-IYNHSRRRSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3647420)

**PubChem compound IDs**

- 51039030

**FDA ingredient codes (UNII)**

- CJN36EQM0H

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

pyrotinib

**Type**

Synthetic organic

**Drug name stem**

\-tinib

**Approval recorded by Guide to Pharmacology**

Yes

### Mechanisms of action (4)

- **Mechanism**  
Epidermal growth factor receptor erbB1 inhibitor

**Action type**  
Inhibitor

**Target**  
Epidermal growth factor receptor

**Protein identifier**  
P00533
- **Mechanism**  
Receptor protein-tyrosine kinase erbB-2 inhibitor

**Action type**  
Inhibitor

**Target**  
Receptor tyrosine-protein kinase erbB-2

**Protein identifier**  
P04626
- **Action**  
Irreversible inhibition

**Action type**  
IRREVERSIBLE\_INHIBITION

**Target**  
epidermal growth factor receptor

**Gene symbol**  
EGFR

**Protein identifier**  
P00533

**Median affinity**

7.89

**Affinity units**  
pIC50
- **Action**  
Irreversible inhibition

**Action type**  
IRREVERSIBLE\_INHIBITION

**Target**  
erb-b2 receptor tyrosine kinase 2

**Gene symbol**  
ERBB2

**Protein identifier**  
P04626

**Median affinity**

7.42

**Affinity units**  
pIC50

### Open Targets mechanisms (2)

- **Mechanism**  
Epidermal growth factor receptor erbB1 inhibitor

**Action type**  
Inhibitor

**Target**  
Epidermal growth factor receptor
- **Mechanism**  
Receptor protein-tyrosine kinase erbB-2 inhibitor

**Action type**  
Inhibitor

**Target**  
Receptor tyrosine-protein kinase erbB-2

### Investigated indications (8)

- **Condition**  
Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Carcinoma, Non-Small-Cell Lung

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003060

**Subject identifier**  
D002289
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003869

**Subject identifier**  
D001943
- **Condition**  
Triple Negative Breast Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0005537

**Subject identifier**  
D064726
- **Condition**  
Digestive System Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0008549

**Subject identifier**  
D004067
- **Condition**  
Stomach Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0001056

**Subject identifier**  
D013274
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0005575

**Subject identifier**  
D015179
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0007254

**Subject identifier**  
D001943

### Open Targets indications (25)

- **Condition identifier**  
EFO\_0000616

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003060

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0003869

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0005922

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0008549

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1000294
- **Condition identifier**  
MONDO\_0000521

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001056

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0003060

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004379
- **Condition identifier**  
MONDO\_0004669
- **Condition identifier**  
MONDO\_0004950

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0004992

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005028

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005061

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005494

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005575

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005580

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0007254

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0007256

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008903

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0009831

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0021040

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0040679

**Highest recorded phase**  
2

### Reported adverse events (25)

- **Event**  
alanine aminotransferase increased

**Reports**  
9

**Reporting signal score**

24.5059
- **Event**  
anaemia

**Reports**  
12

**Reporting signal score**

25.5811
- **Event**  
aspartate aminotransferase increased

**Reports**  
8

**Reporting signal score**

21.6817
- **Event**  
blood bilirubin increased

**Reports**  
3

**Reporting signal score**

8.87439
- **Event**  
decreased appetite

**Reports**  
5

**Reporting signal score**

10.1523
- **Event**  
diarrhoea

**Reports**  
19

**Reporting signal score**

35.2218
- **Event**  
drug resistance

**Reports**  
4

**Reporting signal score**

11.5473
- **Event**  
fatigue

**Reports**  
7

**Reporting signal score**

8.31454
- **Event**  
granulocyte count decreased

**Reports**  
2

**Reporting signal score**

10.3622
- **Event**  
hepatic function abnormal

**Reports**  
4

**Reporting signal score**

10.245
- **Event**  
hypokalaemia

**Reports**  
6

**Reporting signal score**

16.2658
- **Event**  
leukopenia

**Reports**  
6

**Reporting signal score**

15.2867
- **Event**  
metastasis

**Reports**  
5

**Reporting signal score**

24.1175
- **Event**  
mouth ulceration

**Reports**  
3

**Reporting signal score**

8.40937
- **Event**  
myelosuppression

**Reports**  
12

**Reporting signal score**

58.5585
- **Event**  
nausea

**Reports**  
13

**Reporting signal score**

16.0045
- **Event**  
neutropenia

**Reports**  
10

**Reporting signal score**

22.1075
- **Event**  
neutrophil count decreased

**Reports**  
3

**Reporting signal score**

7.97058
- **Event**  
palmar-plantar erythrodysaesthesia syndrome

**Reports**  
9

**Reporting signal score**

34.3669
- **Event**  
pigmentation disorder

**Reports**  
3

**Reporting signal score**

13.1924
- **Event**  
rash

**Reports**  
6

**Reporting signal score**

8.2457
- **Event**  
stomatitis

**Reports**  
6

**Reporting signal score**

16.5146
- **Event**  
thrombocytopenia

**Reports**  
8

**Reporting signal score**

16.608
- **Event**  
transaminases increased

**Reports**  
3

**Reporting signal score**

8.74789
- **Event**  
vomiting

**Reports**  
12

**Reporting signal score**

18.4451

### Trial references (107)

- NCT01937689  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01937689)
- NCT02361112  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02361112)
- NCT02422199  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02422199)
- NCT02500199  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02500199)
- NCT02973737  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02973737)
- NCT03080805  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03080805)
- NCT03412383  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03412383)
- NCT03588091  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03588091)
- NCT03691051  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03691051)
- NCT03735966  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03735966)
- NCT03772353  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03772353)
- NCT03863223  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03863223)
- NCT03876587  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03876587)
- NCT03923166  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03923166)
- NCT03923179  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03923179)
- NCT03980054  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03980054)
- NCT03993964  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03993964)
- NCT03997539  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03997539)
- NCT04001621  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04001621)
- NCT04033172  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04033172)
- NCT04034589  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04034589)
- NCT04066790  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04066790)
- NCT04088110  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04088110)
- NCT04095390  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04095390)
- NCT04126525  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04126525)

And 82 more, listed on the interactive page.

## Chemical properties

**Hydrogen bond acceptors**

8

**Hydrogen bond donors**

2

**Polar surface area**

112.4

**Calculated partition coefficient (ALogP)**

6.47

**Calculated partition coefficient (XLogP)**

5.4

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

2

**Rotatable bonds**

10

**Heavy atoms**

42

**Molecular formula**

C32H31ClN6O3

**Monoisotopic mass**

582.2146166

**Natural product**

No

## Evidence counts

**Recorded assays**

33

**Active assays**

29

### Active assay types (2)

- Confirmatory
- Other

## Related records

### Trials (170)

- 18F-FDG Uptake Heterogeneity Predicts Pyrotinib Response
- A Clinica Study of Pyrotinib in Patients of Advanced Non-Small Cell Lung Cancer With HER2 Mutation
- [A Clinical Study of JS105 in Combination With Other Anti-tumor Therapies in Patients With Solid Tumors](https://trialight.com/data/trial/a-clinical-study-of-js105-in-combination-with-other-anti-a416fdf1-1a18-433c-aa31-f3b60bad7915.md)
- A Clinical Study of Pyrotinib in Patients With HER2-positive Advanced Colorectal Cancer
- A Drug-drug Interaction Trial of Loperamide Pharmacokinetics Effect on Pyrotinib Maleate
- A Phase II Clinical Study of Treatment With Disitamb Vedotin Plus Pyrotinib in HER2-positive Early Breast Cancer
- A Phase II Study of Trastuzumab Deruxtecan (T-DXd) Plus Pyrotinib in HER2-Positive Advanced Breast Cancer After Progression on T-DXd
- A Phase Ⅱ Trial of Pyrotinib Combination With CDK4/6 Inhibitor SHR6390 in Patients Prior Trastuzumab-treated Advanced HER2-Positive Breast Cancer
- A Prospective, Open-label, Exploratory Basket Trial to Evaluate the Efficacy and Safety of Sintilimab Combined With Pyrotinib ± Chemotherapy in Patients With Advanced Digestive System Tumors
- A Prospective, Open, Multicenter Single-arm Clinical Studie of Docetaxel, Carboplatin Combined With Inetetamab and Pyrotinib in the Treatment of Local-advanced HER2-positive Breast Cancer
- A Real-World Study of Pyrotinib Maleate in the Treatment of Advanced/Metastatic Non-Small Cell Lung Cancer With Rare Mutations in HER2
- A Study of ARX788 Combined With Pyrotinib Maleate Versus TCBHP (Trastuzumab Plus Pertuzumab With Docetaxel and Carboplatin) as Neoadjuvant Treatment in HER2-positive Breast Cancer Patients
- A Study of Diarrhea and Intestinal Flora Changes Caused by Pyrotinib in Breast Cancer
- A Study of Evaluating The Effects Of Pyrotinib After Adjuvant Trastuzumab In Women With Early Stage Breast Cancer
- A Study of Neoadjuvant SHR6390 in Combination With Anastrozole, Pyrotinib, and Trastuzumab in Patients With ER+/HER2+ Breast Cancer.
- A Study of Pyrotinib Combined With Capecitabine for Metastatic HER-2 Positive Colorectal Cancer
- A Study of Pyrotinib in Combination With Trastuzumab and Docetaxel in Patients With HER2 Metastatic Breast Cancer
- A Study of Pyrotinib Plus Capecitabine in Patients With Brain Metastases From HER2-positive Metastatic Breast Cancer
- A Study of Pyrotinib Plus Capecitabine in Patients With HER2+ Metastatic Breast Cancer
- A Study of Pyrotinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in Patients With HER2+Metastatic Breast Cancer Who Have Prior Received Anthracyclin, Taxane or Trastuzumab

### In development for (20)

- [Biliary tract cancer](https://trialight.com/data/condition/biliary-tract-cancer-6b9535c9-ccaa-5b47-8c46-0d05d39d7c62.md) Phase 2
- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 3
- [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md) Phase 3
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 2
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 2
- [Digestive system neoplasm](https://trialight.com/data/condition/digestive-system-neoplasm-2ebb9146-1d78-515a-92a3-749515a27d44.md) Phase 2
- [Esophageal adenocarcinoma](https://trialight.com/data/condition/esophageal-adenocarcinoma-4bf4a077-18f0-54cb-9a30-b8ea936afe32.md) Phase 2
- [Esophageal squamous cell carcinoma](https://trialight.com/data/condition/esophageal-squamous-cell-carcinoma-c10bd9c9-02f9-5805-8008-b021f4604e7a.md) Phase 2
- [Gastric cancer](https://trialight.com/data/condition/gastric-cancer-3c1e2785-2672-5b3e-afce-9335f684c159.md) Phase 2
- Gastric carcinoma Phase 1
- [Hepatocellular carcinoma](https://trialight.com/data/condition/hepatocellular-carcinoma-fc1014ac-5a3c-551d-98ea-95306009e299.md) Phase 2
- [Lung adenocarcinoma](https://trialight.com/data/condition/lung-adenocarcinoma-1cff3624-1dd5-5076-89a7-1f8a28c087a6.md) Phase 2
- [Lung cancer](https://trialight.com/data/condition/lung-cancer-c4ca1fe0-9b3d-5957-a668-2d6cf26bd16a.md) Phase 2
- [Malignant pancreatic neoplasm](https://trialight.com/data/condition/malignant-pancreatic-neoplasm-5dd0b53e-5962-50ea-a2e5-cf2444bd0485.md) Phase 2
- [Neoplasm](https://trialight.com/data/condition/neoplasm-2a973797-359b-5982-907e-98f9b7c1a284.md) Phase 2
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 3
- [Pancreatic neoplasm](https://trialight.com/data/condition/pancreatic-neoplasm-de300cc3-339a-5c06-97d8-2d9155fc3a7b.md) Phase 2
- Salivary gland carcinoma Phase 2
- [Triple-negative breast carcinoma](https://trialight.com/data/condition/triple-negative-breast-carcinoma-059174a2-9b5f-5234-90b9-4a4fee6eb9bb.md) Phase 2
- [Urothelial carcinoma](https://trialight.com/data/condition/urothelial-carcinoma-b2aa266d-2d5f-5e5d-a0de-62274f2dc094.md) Phase 2

### Other linked conditions (3)

- Female breast carcinoma
- [HER2 positive breast carcinoma](https://trialight.com/data/condition/her2-positive-breast-carcinoma-eb8493ec-908e-5435-bf56-0d20c0c9bb88.md)
- Salivary gland cancer

### Targets (2)

- [EGFR](https://trialight.com/data/target/egfr-5c134fbe-bf90-5792-81e3-542be53c2be7.md) Epidermal growth factor receptor erbB1 inhibitor
- [ERBB2](https://trialight.com/data/target/erbb2-900ec94b-8cc2-5864-a53d-4b5ed23c71f5.md) Receptor protein-tyrosine kinase erbB-2 inhibitor

---

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