Sacituzumab tirumotecan

Highest phase reached
Drug type
Antibody drug conjugate

Listing at source
Listed
Highest phase reached

Drug type
Antibody drug conjugate
Drug name
Sacituzumab tirumotecan

  • immunoglobulin g1 anti human tumor associated calcium signal transducer 2 human mus musculus monoclonal hrs7 γ1 chain disulfide with human mus musculus monoclonal hrs7 κ chain dimer reduced s 5 6 1 34s 38 amino 34 4 4s 4 ethyl 3 4 12 14 tetrahydro 11 2 1 methylethyl methylsulfonyl amino ethyl 3 14 dioxo 1h pyrano 3 4 6 7 indolizino 1 2 b quinolin 4 yl oxy carbonyl oxy methyl phenyl amino carbonyl 28 32 dioxo 3 6 9 12 15 18 21 24 30 nonaoxa 27 33 diazaoctatriacont 1 yl 1h 1 2 3 triazol 4 yl methyl amino 6 oxo 1 hexyn 1 yl 2 pyrimidinyl l cysteine
  • immunoglobulin g1 kappa anti homo sapiens tacstd2 tumor associated calcium signal transducer 2 membrane component chromosome 1 surface marker 1 m1s1 gastrointestinal tumor associated antigen ga7331 pancreatic carcinoma marker protein ga733 1 epithelial glycoprotein 1 egp 1 trophoblast antigen 2 cell surface glycoprotein trop 2 trop2 humanized monoclonal antibody conjugated to the topoisomerase i inhibitor tirumotecan
  • immunoglobulin g1 kappa anti homo sapiens tacstd2 tumor associated calcium signal transducer 2 membrane component chromosome 1 surface marker 1 m1s1 gastrointestinal tumor associated antigen ga7331 pancreatic carcinoma marker protein ga733 1 epithelial glycoprotein 1 egp 1 trophoblast antigen 2 cell surface glycoprotein trop 2 trop2 humanized monoclonal antibody conjugated to the topoisomerase i inhibitor tirumotecan gamma1 heavy chain humanized 1 451 vh homo sapiens ighv7 4 1 02 85 70 ighd ighj4 01 86 7 t122 s 115 cdr imgt 8 8 14 26 33 51 58 97 110 1 121 homo sapiens ighg1 03 g1m3 ng1m1ch1 r120 ch3 e12 m14 ch1 r120 218 122 219 hinge 220 234 ch2 235 344 ch3 e12 360 m14 362 345 449 chs 450 451 122 451 224 214 disulfide with kappa light chain humanized 1 214 v kappa homo sapiens igkv1 9 01 82 2 igkj4 01 91 7 g120 a 100 cdr imgt 6 3 9 27 32 50 52 89 97 1 107 homo sapiens igkc 01 km3 a45 1 153 v101 191 108 214 dimer 230 230 233 233 bisdisulfide produced in chinese hamster ovary cho cells cell line cho s glycoform alfa substituted at the sulfur atoms of eight l cysteinyl residues with 5 6 1 34s 38 amino 34 4 4s 4 ethyl 11 2 n propan 2 yl methanesulfonamido ethyl 3 14 dioxo 3 4 12 14 tetrahydro 1h pyrano 3 4 6 7 indolizino 1 2 b quinolin 4 yl oxy carbonyl oxy methyl phenyl carbamoyl 28 32 dioxo 3 6 9 12 15 18 21 24 30 nonaoxa 27 33 diazaoctatriacontan 1 yl 1h 1 2 3 triazol 4 yl methyl amino 6 oxohex 1 yn 1 yl pyrimidin 2 yl tirumotecan groups
  • Immunoglobulin G1-kappa, anti-[Homo sapiens TACSTD2 (tumor-associated calcium signal transducer 2, membrane component chromosome 1 surface marker 1, M1S1, gastrointestinal tumor-associated antigen GA7331, pancreatic carcinoma marker protein GA733-1, epithelial glycoprotein-1, EGP-1, trophoblast antigen-2, cell surface glycoprotein Trop-2, TROP2)], humanized monoclonal antibody, conjugated to the topoisomerase I inhibitor tirumotecan
  • immunoglobulin G1-kappa, anti-[Homo sapiens TACSTD2 (tumor-associated calcium signal transducer 2, membrane component chromosome 1 surface marker 1, M1S1, gastrointestinal tumor-associated antigen GA7331, pancreatic carcinoma marker protein GA733-1, epithelial glycoprotein-1, EGP-1, trophoblast antigen-2, cell surface glycoprotein Trop-2, TROP2)], humanized monoclonal antibody; conjugated to the topoisomerase I inhibitor tirumotecan; gamma1 heavy chain humanized (1-451) [VH (Homo sapiens IGHV7-4-1*02 (85.70%) -(IGHD)-IGHJ4*01 (86.7%) T122>S (115), CDR-IMGT [8.8.14] (26-33.51-58.97-110)) (1-121) -Homo sapiens IGHG1*03, G1m3, nG1m1CH1 R120, CH3 E12, M14 (CH1 R120 (218) (122-219), hinge (220-234), CH2 (235-344), CH3 E12 (360), M14 (362) (345-449), CHS (450-451)) (122-451)], (224-214')- disulfide with kappa light chain humanized (1'-214') [V-KAPPA (Homo sapiens IGKV1-9*01 (82.2%) -IGKJ4*01 (91.7%) G120>A (100), CDR-IMGT [6.3.9] (27'-32'.50'-52'.89'-97')) (1'-107') -Homo sapiens IGKC*01, Km3, A45.1 (153'), V101 (191') (108'-214')]; dimer (230-230":233-233")-bisdisulfide, produced in Chinese hamster ovary (CHO) cells, cell line CHO-S, glycoform alfa; substituted at the sulfur atoms of eight L-cysteinyl residues with 5-(6-{[(1-{(34S)-38-amino-34-[(4-{[({[(4S)-4-ethyl-11-{2-[N-(propan-2-yl)methanesulfonamido]ethyl}-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-4-yl]oxy}carbonyl)oxy]methyl}phenyl)carbamoyl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27,33-diazaoctatriacontan-1-yl}-1H-1,2,3-triazol-4-yl)methyl]amino}-6-oxohex-1-yn-1-yl)pyrimidin-2-yl (tirumotecan) groups
  • Immunoglobulin G1, anti-(human tumor-associated calcium signal transducer 2) (human-Mus musculus monoclonal hRS7 γ1-chain), disulfide with human-Mus musculus monoclonal hRS7 κ-chain, dimer, reduced, S-[5-[6-[[[1-[(34S)-38-amino-34-[[[4-[[[[[(4S)-4-ethyl-3,4,12,14-tetrahydro-11-[2-[(1-methylethyl)(methylsulfonyl)amino]ethyl]-3,14-dioxo-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinolin-4-yl]oxy]carbonyl]oxy]methyl]phenyl]amino]carbonyl]-28,32-dioxo-3,6,9,12,15,18,21,24,30-nonaoxa-27,33-diazaoctatriacont-1-yl]-1H-1,2,3-triazol-4-yl]methyl]amino]-6-oxo-1-hexyn-1-yl]-2-pyrimidinyl]-L-cysteine
  • mk 2870
  • Mk-2870
  • mk2870
  • MK2870
  • sacituzumab tirumotecan
  • Sacituzumab tirumotecan
  • Sacituzumab Tirumotecan
  • Sacituzumab Tirumotecan (Observational Cohort)
  • Sacituzumab tirumotecan (sac-TMT)
  • Sacituzumab Tirumotecan (sac-TMT)
  • Sacituzumab Tirumotecan (Sac-TMT)
  • Sacituzumab Tirumotecan (SKB264)
  • sacituzumab tirumotecan [INN]
  • SACITUZUMAB TIRUMOTECAN [USAN]
  • Sacituzumab tirumotecan [WHO-DD]
  • sacituzumab tirumotecan inn
  • sacituzumab tirumotecan usan
  • sacituzumab tirumotecan who dd
  • skb 264

And 4 more, listed on the interactive page.

CAS registry numbers
  • 2768350-77-0
ChEMBL ID
CHEMBL5314875
FDA ingredient codes (UNII)
  • 3DV5TD1VL3

First in class
No
Orphan designation
No

Pharmacology name
sacituzumab tirumotecan
Type
Antibody
Drug name stem
-mab; -mab; -tecan
Approval recorded by Guide to Pharmacology
Yes

Mechanisms of action

  • Action
    Binding
    Action type
    Binding
    Target
    tumor associated calcium signal transducer 2
    Gene symbol
    TACSTD2
    Protein identifier
    P09758
    Median affinity
    9.51
    Affinity units
    pKd

  • 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
    Esophageal Neoplasms
    Highest recorded phase
    1
    Condition identifier
    EFO:0005922
    Subject identifier
    D004938
  • Condition
    Urinary Bladder Neoplasms
    Highest recorded phase
    1
    Condition identifier
    EFO:0008528
    Subject identifier
    D001749
  • Condition
    Uterine Cervical Neoplasms
    Highest recorded phase
    3
    Condition identifier
    MONDO:0002974
    Subject identifier
    D002583
  • Condition
    Breast Neoplasms
    Highest recorded phase
    3
    Condition identifier
    MONDO:0007254
    Subject identifier
    D001943
  • Condition
    Endometrial Neoplasms
    Highest recorded phase
    3
    Condition identifier
    MONDO:0011962
    Subject identifier
    D016889

  • Condition identifier
    EFO_0000616
    Highest recorded phase
    2
  • Condition identifier
    EFO_0003060
    Highest recorded phase
    3
  • Condition identifier
    EFO_0005537
    Highest recorded phase
    3
  • Condition identifier
    EFO_1000576
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0000521
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0002447
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0002974
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0003219
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0004971
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0004992
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005028
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0005036
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0005070
  • Condition identifier
    MONDO_0005075
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005140
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005153
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005233
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0005494
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0005580
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0006082
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0006260
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0006382
  • Condition identifier
    MONDO_0006451
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0006468
  • Condition identifier
    MONDO_0007254
    Highest recorded phase
    3

And 12 more, listed on the interactive page.

  • Event
    anaemia
    Reports
    16
    Reporting signal score
    12.7972
  • Event
    chemotherapy cytokine prophylaxis
    Reports
    1
    Reporting signal score
    9.02064
  • Event
    chemotherapy side effect prophylaxis
    Reports
    1
    Reporting signal score
    8.32754
  • Event
    colitis
    Reports
    7
    Reporting signal score
    11.3782
  • Event
    cytopenia
    Reports
    4
    Reporting signal score
    8.6995
  • Event
    dairy intolerance
    Reports
    2
    Reporting signal score
    12.9169
  • Event
    diarrhoea
    Reports
    26
    Reporting signal score
    13.7248
  • Event
    discontinued product administered
    Reports
    2
    Reporting signal score
    11.9114
  • Event
    disease progression
    Reports
    38
    Reporting signal score
    90.4906
  • Event
    disseminated varicella
    Reports
    1
    Reporting signal score
    6.71846
  • Event
    enteritis
    Reports
    4
    Reporting signal score
    10.6055
  • Event
    febrile neutropenia
    Reports
    24
    Reporting signal score
    51.1387
  • Event
    neutropenia
    Reports
    30
    Reporting signal score
    48.8089
  • Event
    neutropenic colitis
    Reports
    8
    Reporting signal score
    36.3007
  • Event
    neutrophil count abnormal
    Reports
    5
    Reporting signal score
    18.0419
  • Event
    neutrophil count decreased
    Reports
    17
    Reporting signal score
    38.5591
  • Event
    sepsis
    Reports
    7
    Reporting signal score
    6.77128
  • Event
    skin tightness
    Reports
    3
    Reporting signal score
    10.0936
  • Event
    therapy change
    Reports
    4
    Reporting signal score
    10.5383
  • Event
    triple negative breast cancer
    Reports
    2
    Reporting signal score
    10.3495
  • Event
    ureteric obstruction
    Reports
    2
    Reporting signal score
    6.79728
  • Event
    white blood cell count decreased
    Reports
    14
    Reporting signal score
    17.3864
  • Event
    wound infection bacterial
    Reports
    2
    Reporting signal score
    9.92988

Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Natural product
No

  • Component
    Glycosylation sites (N)
    Sequence
    301 $ 301''
  • Component
    Heavy chain
    Type
    Protein
    Sequence
    QVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTYTDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
  • Component
    Light chain
    Type
    Protein
    Sequence
    DIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPDRFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
  • Component
    Disulfide bridges
    Sequence
    22-96 $ 22''-96'' $ 23'-88' $ 23'''-88''' $ 134'-194' $ 134'''-194''' $ 148-204 $ 148''-204'' $ 224-214' $ 224''-214''' $ 230-230'' $ 233-233'' $ 265-325 $ 265''-325'' $ 371-429 $ 371'-429''

Related records

Trials (105)

In development for (10)