Trastuzumab envedotin

Highest phase reached
Drug type
Antibody drug conjugate

Listing at source
Listed
Highest phase reached

Drug type
Antibody drug conjugate
Drug name
Trastuzumab envedotin

  • arm 1 sirolimus for injection albumin bound dp303c
  • dp 303c
  • DP-303C
  • dp303c
  • Dp303c
  • DP303c
  • DP303c injection
  • h gamma1 heavy chain humanized 1 450 vh homo sapiens ighv3 66 01 81 6 ighd ighj4 01 100 cdr imgt 8 8 13 26 33 51 58 97 109 1 120 homo sapiens ighg1 03v g1m3 g1m17 ng1m1 ch1 k120 ch3 e12 m14 ch1 r120 k 217 121 218 hinge 1 15 219 233 ch2 234 343 ch3 e12 359 m14 361 344 448 chs 449 450 121 450 223 214 disulfide with l kappa light chain humanized 1 214 v kappa homo sapiens igkv1 39 01 86 3 igkj1 01 100 cdr imgt 6 3 9 27 32 50 52 89 97 1 107 homo sapiens igkc 01 100 km3 a45 1 153 v101 191 108 214 dimer 229 229 232 232 bisdisulfide produced in chinese hamster ovary cho cells glycoform alfa substituted at the side chain nitrogen atom of l glutaminyl residues 298 and 298 with a radical group consisting of 6s 9s 1 amino 6 4 5s 8s 11s 12r 11 2s butan 2 yl 12 2 2s 2 1r 2r 3 1s 2r 1 hydroxy 1 phenylpropan 2 yl amino 1 methoxy 2 methyl 3 oxopropyl pyrrolidin 1 yl 2 oxoethyl 4 10 dimethyl 3 6 9 trioxo 5 8 di propan 2 yl 2 13 dioxa 4 7 10 triazatetradecyl phenyl carbamoyl 1 8 11 trioxo 9 propan 2 yl 13 16 19 trioxa 2 7 10 triazahenicosan 21 yl envedotin
  • H-gamma1 heavy chain humanized (1-450) [VH (Homo sapiens IGHV3-66*01 (81.6%) -(IGHD) -IGHJ4*01 (100%), CDR-IMGT [8.8.13] (26-33.51-58.97-109)) (1-120) -Homo sapiens IGHG1*03v, G1m3>G1m17, nG1m1 CH1 K120, CH3 E12, M14 (CH1 R120>K (217) (121-218), hinge 1-15 (219-233), CH2 (234-343), CH3 E12 (359), M14 (361) (344-448), CHS (449-450)) (121-450)], (223-214')-disulfide with L-kappa light chain humanized (1'-214') [V-KAPPA (Homo sapiens IGKV1-39*01 (86.3%) -IGKJ1*01 (100%), CDR-IMGT [6.3.9] (27'-32'.50'-52'.89'-97')) (1'-107') -Homo sapiens IGKC*01 (100%), Km3 A45.1 (153'), V101 (191') (108'-214')]; dimer (229-229'':232-232'')-bisdisulfide, produced in Chinese hamster ovary (CHO) cells, glycoform alfa; substituted at the side chain nitrogen atom of L-glutaminyl residues 298 and 298'' with a radical group consisting of (6S,9S)-1-amino-6-({4-[(5S,8S,11S,12R)-11-[(2S)-butan-2-yl]-12-(2-{(2S)-2-[(1R,2R)-3-{[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-2-oxoethyl)-4,10-dimethyl-3,6,9-trioxo-5,8-di(propan-2-yl)-2,13-dioxa-4,7,10-triazatetradecyl]phenyl}carbamoyl)-1,8,11-trioxo-9-(propan-2-yl)-13,16,19-trioxa-2,7,10-triazahenicosan-21-yl (envedotin)
  • immunoglobulin g1 anti human epidermal growth factor receptor her2 human mus musculus monoclonal dp001 γ1 chain disulfide with human mus musculus monoclonal dp001 κ chain dimer 298 298 diamide with n 4 n 2 2 2 2 aminoethoxy ethoxy ethoxy acetyl l valyl n5 aminocarbonyl l ornithyl amino phenyl methoxy carbonyl n methyl l valyl n 1s 2r 4 2s 2 1r 2r 3 1r 2s 2 hydroxy 1 methyl 2 phenylethyl amino 1 methoxy 2 methyl 3 oxopropyl 1 pyrrolidinyl 2 methoxy 1 1s 1 methylpropyl 4 oxobutyl n methyl l valinamide
  • immunoglobulin g1 kappa anti homo sapiens erbb2 receptor tyrosine protein kinase erbb 2 epidermal growth factor receptor 2 egfr2 her2 her 2 p185c erbb2 neu cd340 humanized monoclonal antibody conjugated at glutaminyl residues to monomethylauristatin e mmae with a ratio of 1 to 2 via a cleavable linker
  • immunoglobulin G1-kappa, anti-[Homo sapiens ERBB2 (receptor tyrosine-protein kinase erbB-2, epidermal growth factor receptor 2, EGFR2, HER2, HER-2, p185c-erbB2, NEU, CD340)], humanized monoclonal antibody, conjugated at glutaminyl residues to monomethylauristatin E (MMAE), with a ratio of 1 to 2, via a cleavable linker
  • Immunoglobulin G1, anti-(human epidermal growth factor receptor HER2) (human-Mus musculus monoclonal DP001 γ1-chain), disulfide with human-Mus musculus monoclonal DP001 κ-chain, dimer, 298,298′-diamide with N-[[[4-[[N-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]acetyl]-L-valyl-N5-(aminocarbonyl)-L-ornithyl]amino]phenyl]methoxy]carbonyl]-N-methyl-L-valyl-N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide
  • trastuzumab envedotin
  • Trastuzumab envedotin
  • trastuzumab envedotin [INN]
  • trastuzumab envedotin inn
  • trastuzumab envedotina
  • Trastuzumab envedotina
  • trastuzumab envedotine
  • Trastuzumab envedotine

CAS registry numbers
  • 2865132-89-2
ChEMBL ID
CHEMBL6068184
FDA ingredient codes (UNII)
  • 37DMF82G1F

First in class
No
Orphan designation
No

Drug name stem
-dotin; -mab; -mab

  • Condition
    Neoplasms
    Highest recorded phase
    2
    Condition identifier
    EFO:0000616
    Subject identifier
    D009369
  • Condition
    Breast Neoplasms
    Highest recorded phase
    3
    Condition identifier
    MONDO:0007254
    Subject identifier
    D001943

  • Condition identifier
    EFO_0000616
  • Condition identifier
    EFO_1000294
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0001056
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0003219
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005036
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005070
  • Condition identifier
    MONDO_0007254
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0008170
    Highest recorded phase
    2

Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Natural product
No

  • Component
    Heavy chain
    Type
    Protein
    Sequence
    EVQLVESGGGLVQPGGSLRLSCAASGENIKDTYTHWVRQAPGKGLEWVARIYPTNGYTRYADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGEYAMDYWGQGTLVTVSSASTKGPSVEPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGPSVFLEPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKENWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPBNNYKTTPPVLDSDGSFFLYSKLTVDKSRWQGNVEFSCSVMHEALHNHYTQKSLSLSPGK
  • Component
    Disulfide bridges
    Sequence
    22-96 $ 22''-96'' $ 23'-88' $ 23'''-88''' $ 134'-194' $ 134'''-194''' $ 147-203 $ 147''-203'' $ 223-214' $ 223''-214''' $ 229-229'' $ 232-232''$ 264-324 $ 264''-324'' $ 370-428 $ 370''-428''
  • Component
    Light chain
    Type
    Protein
    Sequence
    DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPSRESGSRSGTDFTLTISSLQPBDEFATYYCQHYTTPPTEGQGTKVELKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSENRGEC
  • Component
    Glycosylation sites (N)
    Sequence
    300 $ 300''

Related records

Trials (8)

In development for (3)