Petosemtamab

Highest phase reached
Drug type

Listing at source
Listed
Highest phase reached

Drug type
Drug name
Petosemtamab

  • 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

CAS registry numbers
  • 2213450-26-9
ChEMBL ID
CHEMBL4297781
FDA ingredient codes (UNII)
  • Z6Z6IVE7W4

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 name
petosemtamab
Type
Antibody
Drug name stem
-mab

  • 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

  • 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

Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Natural product
No

  • 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)

In development for (6)

Targets (2)