> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/petosemtamab-661ba63c-03d6-4a61-bfb8-83dbf0a9cf89
> Record changed: 2026-11-04

# Petosemtamab

Highest phase reached

Phase 1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297781)

Drug type

Antibody

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297781)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297781)

## Names and chemistry

**Drug type**

Antibody

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297781)

**Drug name**

Petosemtamab

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297781)

### Other names (20)

- Immunoglobulin G1 \[361-lysine, 376-lysine\], anti-(human leucine-rich repeat-containing G protein-coupled receptor LGR5) (human monoclonal MCLA-158 γ1-chain), disulfide with human monoclonal MCLA-158 κ-chain, (236→229'), (239→232')-bis(disulfide) with immunoglobulin G1 \[354-aspartic acid, 371-glutamic acid\] anti-(human epidermal growth factor receptor) (human monoclonal MCLA-158 γ1-chain) disulfide with human monoclonal MCLA-158 κ-chain
- immunoglobulin g1 361 lysine 376 lysine anti human leucine rich repeat containing g protein coupled receptor lgr5 human monoclonal mcla 158 γ1 chain disulfide with human monoclonal mcla 158 κ chain 236 229 239 232 bis disulfide with immunoglobulin g1 354 aspartic acid 371 glutamic acid anti human epidermal growth factor receptor human monoclonal mcla 158 γ1 chain disulfide with human monoclonal mcla 158 κ chain
- immunoglobulin g1 kappa anti homo sapiens egfr epidermal growth factor receptor receptor tyrosine protein kinase erbb 1 erbb1 her1 her 1 erbb and anti homo sapiens lgr5 leucine rich repeat containing g protein coupled receptor 5 g protein coupled receptor 49 gpr67 gpr49 homo sapiens monoclonal antibody bispecific heterodimeric gamma1 heavy chain homo sapiens anti egfr 1 449 vh homo sapiens ighv7 4 1 02 91 8 ighd ighj4 01 93 3 8 8 13 1 120 homo sapiens ighg1 03 100 g1m3 ng1m1 ch1 r120 217 121 218 hinge 1 15 219 233 ch2 234 343 ch3 l7 d 354 e12 359 m14 361 l24 e 371 344 448 chs k2 del 449 121 449 223 214 disulfide with kappa light chain homo sapiens 1 214 v kappa homo sapiens igkv1 39 01 100 igkj1 01 100 6 3 9 1 107 homo sapiens igkc 01 100 km3 a45 1 153 v101 191 108 214 gamma1 heavy chain homo sapiens anti lgr5 1 456 vh homo sapiens ighv7 4 1 01 92 9 ighd ighj4 01 93 3 8 8 20 1 127 homo sapiens ighg1 03 100 g1m3 ng1m1 ch1 r120 224 128 225 hinge 1 15 226 240 ch2 241 350 ch3 l7 k 361 e12 366 m14 368 t22 k 376 351 455 chs k2 del 456 128 456 230 214 disulfide with kappa light chain homo sapiens 1 214 v kappa homo sapiens igkv1 39 01 100 igkj1 01 100 6 3 9 1 107 homo sapiens igkc 01 100 km3 a45 1 153 v101 191 108 214 dimer 229 236 232 239 bisdisulfide produced in chinese hamster ovary cho cells glycoform alfa
- immunoglobulin G1-kappa, anti-\[Homo sapiens EGFR (epidermal growth factor receptor, receptor tyrosine-protein kinase erbB-1, ERBB1, HER1, HER-1, ERBB)\], and anti-\[Homo sapiens LGR5 (leucine rich repeat containing G protein-coupled receptor 5, G protein-coupled receptor 49, GPR67, GPR49)\], Homo sapiens monoclonal antibody, bispecific heterodimeric; gamma1 heavy chain Homo sapiens anti-EGFR (1-449) \[VH (Homo sapiens IGHV7-4-1\*02 (91.8%) -(IGHD) -IGHJ4\*01 (93.3%)) \[8.8.13\] (1-120) -Homo sapiens IGHG1\*03 (100%), G1m3, nG1m1 (CH1 R120 (217) (121-218), hinge 1-15 (219-233), CH2 (234-343), CH3 L7>D (354), E12 (359), M14 (361), L24>E (371) (344-448), CHS K2>del (449)) (121-449)\], (223-214')-disulfide with kappa light chain Homo sapiens (1'-214') \[V-KAPPA (Homo sapiens IGKV1-39\*01 (100%) -IGKJ1\*01 (100%)) \[6.3.9\] (1'-107') -Homo sapiens IGKC\*01 (100%), Km3 A45.1 (153), V101 (191) (108’-214’)\]; gamma1 heavy chain Homo sapiens anti-LGR5 (1-456) \[VH (Homo sapiens IGHV7-4-1\*01 (92.9%) -(IGHD) -IGHJ4\*01 (93.3%)) \[8.8.20\] (1-127) -Homo sapiens IGHG1\*03 (100%), G1m3, nG1m1 (CH1 R120 (224) (128-225), hinge 1-15 (226-240), CH2 (241-350), CH3 L7>K (361), E12 (366), M14 (368), T22>K (376) (351-455), CHS K2>del (456)) (128-456)\], (230-214')-disulfide with kappa light chain Homo sapiens (1'-214') \[V-KAPPA (Homo sapiens IGKV1-39\*01 (100%) -IGKJ1\*01 (100%)) \[6.3.9\] (1'-107') -Homo sapiens IGKC\*01 (100%), Km3 A45.1 (153), V101 (191) (108’-214’)\]; dimer (229-236'':232-239'')-bisdisulfide, produced in Chinese Hamster Ovary (CHO) cells, glycoform alfa
- mcla 158
- mcla 158 folfox
- mcla 158 pembrolizumab
- Mcla-158
- MCLA-158
- mcla158
- MCLA158
- petosemtamab
- Petosemtamab
- petosemtamab \[INN\]
- PETOSEMTAMAB \[USAN\]
- Petosemtamab \[WHO-DD\]
- petosemtamab inn
- petosemtamab pembrolizumab
- petosemtamab usan
- petosemtamab who dd

## Identifiers

**CAS registry numbers**

- 2213450-26-9

**ChEMBL ID**

CHEMBL4297781

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297781)

**FDA ingredient codes (UNII)**

- Z6Z6IVE7W4

## Regulatory information

### Other regulatory facts

**Patents**

0

**Designations**

1

**First in class**

No

**Fast track**

No

**Breakthrough designation**

Yes

**Orphan designation**

No

**Priority review**

No

**Orphan exclusivity**

No

**Accelerated approval**

No

## Pharmacology

### Drug classification

**Pharmacology name**

petosemtamab

**Type**

Antibody

**Drug name stem**

\-mab

### Mechanisms of action (2)

- **Action**  
Binding

**Action type**  
Binding

**Target**  
LGR5

**Gene symbol**  
LGR5

**Protein identifier**  
O75473

**Median affinity**

9.18

**Affinity units**  
pKd
- **Action**  
Binding

**Action type**  
Binding

**Target**  
epidermal growth factor receptor

**Gene symbol**  
EGFR

**Protein identifier**  
P00533

**Median affinity**

9.66

**Affinity units**  
pKd

### Investigated indications

- **Condition**  
Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369

### Open Targets indications (8)

- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_1001480

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005036

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005070
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0006047

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0010150

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0019086

**Highest recorded phase**  
1

## Chemical properties

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Natural product**

No

### Sequences (6)

- **Component**  
Heavy chain: (MF3755)

**Type**  
Protein

**Sequence**  
QVQLVQSGSELKKPGASVKISCKASGYDFTNYAMNWVRQAPGHGLEWMGWINANTGDPTYAQGFTGRFVFSLDTSVSTAYLQISSLKAEDSAVYYCTRERFLEWLHFDYWGQGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTDPPSREEMTKNQVSLTCEVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG
- **Component**  
Heavy chain: (MF5816)

**Type**  
Protein

**Sequence**  
EVQLVQSGSKLKKPGASVKVSCKASGYTFTSYTMNWVRQAPGQGLEWMGWINTDTGDPTYAQGFTGRFVFSLDTSVSTAFLQINSLKAEDTAVYYCARGDCDSTSCYRYSYGYEDYWGQGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTKPPSREEMTKNQVSLKCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG
- **Component**  
Glycosylation sites (N)

**Sequence**  
300 $ 307''''
- **Component**  
Glycosylation sites (N)

**Sequence**  
300 $ 307''
- **Component**  
Disulfide bridges

**Sequence**  
22-96 $ 22''-96''' $ 23'-88' $ 23'''-88''' $ 101''-106'' $ 134'-194' $ 134'''-194'' $ 147-203 $ 154''-210'' $ 223-214' $ 230''-214''' $ 264-324 $ 271''-331'' $ 370-428 $ 377''-435''
- **Component**  
Light chain

**Type**  
Protein

**Sequence**  
DIQMTQSPSSLSASVGDRVTITCRASQSISSYLNWYQQKPGKAPKLLIYAASSLQSGVPSRFSGSGSGTDFTLTISSLQPEDFATYYCQQSYSTPPTFGQGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC

## Related records

### Trials (6)

- A Phase 3 Study to Evaluate Petosemtamab Compared With Investigator's Choice Monotherapy in Previously Treated Head and Neck Squamous Cell Carcinoma Patients (LiGeR-HN2)
- A Phase 3 Study to Evaluate Petosemtamab Plus Pembrolizumab vs Pembrolizumab in First-line Treatment of Head and Neck Cancer (LiGeR - HN1)
- A Study of Bispecific Antibody MCLA-158 in Patients With Advanced Solid Tumors
- Study of Petosemtamab Plus Chemotherapy Versus Cetuximab or Bevacizumab Plus Chemotherapy in RAS and BRAF Wild Type, Recurrent, Unresectable or Metastatic Colorectal Cancer (LiGeR-CRC2)
- [Study of Petosemtamab Plus Chemotherapy Versus Cetuximab Plus Chemotherapy in RAS and BRAF Wild-type, Unresectable or Metastatic, Left-sided Colorectal Cancer (LiGeR-CRC1)](https://trialight.com/data/trial/study-of-petosemtamab-plus-chemotherapy-versus-cetuximab-964c0b27-9b27-451c-956a-7c117ada623b.md)
- Study to Investigate Petosemtamab in Adults With Metastatic Non-Small Cell Lung Cancer

### In development for (6)

- Carcinoma of esophagus Phase 1
- [Gastric adenocarcinoma](https://trialight.com/data/condition/gastric-adenocarcinoma-6bb74a55-7ba6-53e3-a113-22296a84d6ae.md) Phase 1
- [Head and neck squamous cell carcinoma](https://trialight.com/data/condition/head-and-neck-squamous-cell-carcinoma-cbc3ae58-4a6c-52e4-a41b-274051db19fa.md) Phase 3
- [Neoplasm](https://trialight.com/data/condition/neoplasm-2a973797-359b-5982-907e-98f9b7c1a284.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 2
- [Pancreatic adenocarcinoma](https://trialight.com/data/condition/pancreatic-adenocarcinoma-fd65444c-0bc5-53ed-8c6a-62d9809145d0.md) Phase 1

### Targets (2)

- [EGFR](https://trialight.com/data/target/egfr-5c134fbe-bf90-5792-81e3-542be53c2be7.md)
- [LGR5](https://trialight.com/data/target/lgr5-eb2cf1eb-2d55-5b2c-aad6-6bbd3e4b192d.md)

---

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