Product News | Panoramic Layout of ADC Drug Toxins and Linkers

Launched&Registered

Phase 2 Clinical

Phase 1 Cliical

Toxin types

Number of pipelines

Toxin types

Number of pipelines

Toxin types

Number of pipelines

MMAE

3

MMAE

10

MMAE

9

calicheamicin

2

DM1

2

DM1

4

IR700

1

DM4

2

DM4

2

MMAE

1

DXd

2

SG3199

2

SG3199

1

Pseudomonas exotoxin A

2

212Pb

1

DM1

1

tubulysin

2

alpha-emitting radionuclides

1

DXd

1

A-1677770

1

Amberstain

1

MMAF

1

Actnium-225(Ac 225)radiolabelled to satetraxetan

1

Auristatin DolaLock payload

1

PE-38

1

Amanitin

1

Auristatin-0101

1

SN-38

1

anthracycline-derivat ive PNU-159682

1

calicheamicin

1

159682

yttrium-90

1

Auristatin derivative

1

camptothecin

1

Pre-registration&Phase 3

Auristain F-HPA

1

clezutoclax

1

Toxin types

Number of pipelines

belotecan-derived payload

alpha-emitting radioisotopethorium Th 227

1

1

DM1

1

DGN-549

1

deBouganin

1

DM4

2

DOS47

1

DGN-549

1

DXd

1

DT390

1

dibenzocyclooctyne(DBCO)
noncleavable linker

1

MMAF

1

duostatin-5

1

DM-21

1

Ricin Toxin A(RTA)

1

eribulin

1

Duocam ycin analogues

1

staphylococcalenterotoxin A

1

glucocortcoid receptor modulator steroid

1

duostain-5

1

vc-seco-DUBA

1

IL-12

1

engineered transglutaminase，presumed to be derived from trastuzumab and MMAE

1

Pseudomonas exotoxin

1

oxyntomodulin

1

exatecan derivative

1

A

Phase 1 Clinical

PE-38

1

MAAA-1181a

1

Toxin types

Number of pipelines

Pyrrolo benzodiazepine(PBD) dimer

1

maytansine

1

Pyrrolo benzodiazepine(PBD) dimer

1

seco-DUocarmycin hydroxy Benzamide Aza indole(DUBA)

1

Maytansoid

1

pyrrolo benzodiazepine(PBD)) dimerS GD-1882

1

SG3199

1

MMAF

1

SHR 152852

1

TLR 7/ 8 agonist

1

Morphotek's eribulin-linker payload

1

TLR7 agonist

1

truncated diphtheria toxin

1

novel, proprietary， N-acylsulfonamide a uri stat n cytotoxin

1

TLR8 agonist

1

proprietary cleavable drug-linker
1

1

Tub196

1

pyrrolobenzodiazepine(PBD)

1

Preclinical

Toxin types

Number of pipelines

Toxin types

Number of pipelines

Toxin types

Number of pipelines

MMAE

15

DGN-549

1

DGN-549

1

Amanitin

diethylene tri amine penta acetic acid

diethylene triamine pentaaceic acid andy trium-90-1abelled anti-integrin-alpha 6/beta 4(90YITGA6B 4)

5

andy trium-90-1abelledani-integrin-alpha 6/beta 4(90Y-ITGA6B 4)

1

1

DM1

5

dimeric pyrrolo benzodiazepine；dPBD

1

dimeric pyurolo benzodiazepine；d PBD

1

IR700

4

dimeric structure of cyclopropyl pyrrolo[e] indolones(CPI)

1

dimeric structure of cyclopropyi pyrrolo[e] indol ones(CP)

1

PNU-159682

4

DM3/DM4

1

DM3/DM4

1

maytansine

3

DM4/DGN-549

1

DM4/DGN-549

1

SN-38

3

DNA toxin

1

DNA toxin

1

de-immunized antigen-seeding engineered toxin body(ETB)

2

docetaxel

docetaxel

1

1

DGN-462

2

dolastoxin derivate DU 0-5

1

dolastoxin derivate DUO-5

1

doxorubicin

2

DUO-5

1

DUO-5

1

kinesin spindle protein inhibitor

2

duocarmycin derivative

1

duocarmycin derivative

1

maytansinoid

2

duostatin 5.2

1

duostatin 5.2

1

microtubule polymerization  inhibitor

2

PM-050489

1

PM-050489

1

MMAF

2

PM160057

1

PM160057

1

Pseudomonas exotoxin A(PE24)

2

PNU payload

1

PNU payload

1

TLR7/ 8 agonist

2

proprietary MDR-resistantmaytansinoid linker-payload

1

proprietary MDR-resistant maytans in oid linker-payload

1

TLR8 agonist

2

PSARlink hydrophilic drug-linker

1

PSA R link hydrophilic drug-linker

1

tubulysin

2

Pyrrolo benzodiazepine(PBD) dimer

1

Pyrrolo benzodiazepine(PBDdimer

1

alpha emitter thorium-227

1

pyrrolo benzodiazepine(PBD)prodrug

1

pyrrolo benzodiazepine(PBD)prodrug

1

Angio Pep-2

1

pyrrolobenzodiazepine dimer，cyclopropabenz indolone dimer，cyclo propabenzindolone-pyrrolobenzodiazepine heterodimer

pyrrolo benzodiazepine dimer，cyclo propa benzindolone dimer，cyclopropabenzindo lone-pyrrolo benzodiazepineheterodimer

1

1

an-microbial， cell-killing peptid

1

saporin

1

saporin

1

AraLinker-P ABC-MMAE

1

SG3249

1

SG3249

1

Auristatin

1

Shiga-1ike toxin A subunit

1

Shiga-like toxin A subunit

1

Auristatin analogS HR-152852

1

SMCC-DMl and sS PDB-DM 4

1

SMCC-DM1 and sSPDB-DM4

1

Auristatin E

1

soluble MGAA duocar mycin derivative

1

soluble MGAA duocar mycin derivative

1

Auristatin F

1

spliceostatin

1

spliceostatin

1

bouganin

1

thioether 1inker(Zt/g 4-maytansinoid) or via a dipeptide linker to MMAE(Zt/g4-MMAE)

1

thioether 1inker(Zt/g 4may tans in oid) or via a dipeptde linker toM MAE(Zt/g 4-M MAE)

1

chloromethyl benz-indoline dimers，including TP-28

1

deBouganin

1

deimmunized bouganin

1

CLB-SN-38

1

Concortis linker-Duo 5.2toxin

1

cyclopropyrrolonaolit payload

NO

Toxin

Number of pipelines

1

MMAE

39

2

DM1

13

3

Amanitin

6

4

DM4

6

5

PNU-159682

6

6

IR700

5

7

MMAF

5

8

DXd

4

9

maytansine

4

10

SN-38

4

11

tubulysin

4

12

SG3199

4

13

calicheamicin

3

14

DGN-549

3

15

PE-38

3

16

Pseudomonas exotoxin A

3

17

Pyrrolobenzodiazepine(PBD) dimer

3

18

TLR7/8 agonist

3

19

TLR8 agonist

3

20

deBouganin

2

Stage

Toxins TOP 3

Number of pipelines

Phase 3

DM4

2

staphylococcal enterotoxin A、DM1、Ricin Toxin A、MMAF、DXd、vc-seco-DUBA

1

Phase 2

MMAE

10

Tubulysin、Pseudomonas exotoxin A、eribulin、DM1、DM4

2

Phase 1

MMAE

9

DM1

4

DM4、SG3199

2

Preclinical

MMAE

15

Amanitin、DM1、PNU-159682

5

IR700

4

Launched&Registered

Phase 2 Clinical

Phase l Clinical

Phase 2 Clinical

Type of linker

Number of pipelines

Type of linker

Number of pipelines

Type of linker

Number of pipelines

Type of linker

Number of pipelines

mc-val-cit-PABC

3

Cleavable vane-citrulline linker

4

cleavable linker

4

Cleavable vaine-citrulline linker

4

acid-1abile 4(4- acetyl butyrate) linker

1

cleavable linker

3

Cleavable valine-cit rull ne linker

4

non-cleavable linker

3

bifunction a 14( 4 acetyl phenoxy) but an oic acid(Ac Buf)

1

mc-val-cit-PABC

2

SMCC

2

SMCC

3

Cleavable valine-ci tru lie linker

1

non-cleavable linker

2

4APnon-cleavable ln ker

1

cleavable linker

2

hydrolysable carbonate linker

1

peptide linker

2

amide bond

1

non-polyethylene glycol linker

2

MC-Vc-PA Blinker

1

SPDB linker

2

cathepsin cleavable linker

1

sortasemediated antibody conjug ation technology(SMAC)

2

noncleavable maleinidoc aproyl (mc) linker

cathepsin cleavable inker

1

cathepsin- cleavable maleimdocapr oyl-valine-alanine(MC-Val-Ala) type linker

1

bioresversible linker

1

1

SMCC

1

cleavable， valine-alanine dipeptide(as cathepsin eBc leav age site) male ii de type linker containing a spacer PEG

1

cleavable(valine-alanine dipeptide as cathepsin e

1

cathepsin B-cleavable linker

1

B cleavage site) maleimide type linker

tetrapept de linker， Gly-Phe-Leu-Gly(GF LG)

1

cysteine protease-cleavable dipeptide linker

1

Cleavable valine-citr uline-seco(vc-seco)

1

cathepsin B-sensitive cleavable linker

1

tiuxetan

1

flexible PEG lin ker

1

LegoChem ls proprietary linker

1

CL2A linker

1

leavable(valine-alanine dipeptide as cathepsin e B cleavage site) malein ide type linker containing a space rPEG(n=8)

1

furin cleavable linker(RVRR)

1

maytansinoid

1

cleavable disulfide linker

1

Pre-registration&Phase 3

noncleavable maleimidocapr oyl(mc) 1inker

1

maytansin oid inker-payload(DM 21-C)

1

cleavable male imi do-caproylvaecitrulne-para amino benzyl carbamoy 1 linkers

1

Type of linker

Number of pipelines

N-succiniidy 1[4-iodo acetyl] amninobenzoate(SIAB)

1

mc-val-cit-P ABC

1

disulfde bond

1

SPDB linker

2

peptide cleavable linker

1

non-cleavable dibenzo cyclo oc tyne(DB CO) linker

1

disulfide bond to residual cysteine

1

MCC

1

Site-specific Thio Bridge Linker

1

non-polyethylene glycol linker

1

engineered cysteine conjugation

1

PEG spacer

1

SMCC

1

PEGylated gluco ronde linker

1

Ik suda's proprietary PermaLink

1

tetrapeptide-based inker

1

Synthon cleavable linker

1

peptide like r

1

1egu main-cleavable linker

1

proprietary cleavable ln ker

1

LX linker

1

protease-cleavable linker

1

maleimidocaproylvaline citru line pa mino benzyloxy carbonyl

1

smart linker

1

Mersana Therapeut cs'Dol alexin Fleximer linker

1

tetra pept de-based cleavable linker

1

non-cleavable amide/peptide linker

1

uncleavable linker

1

non-cleavable peptide linker

1

novel peptide linker

1

PermaLink conjugation

1

quaternary amine linkers

1

unique lysine conjugation approach

1

NO

Linker

Number of pipelines

1

Cleavable valine-citrullne linker

13

2

deavable linker

9

3

SMCC

7

4

mc-val-cit-PABC

7

5

non-cleavable linker

5

6

SPDB linker

4

7

non-polyethylene glycol linker

3

8

peptide linker

3

9

cathepsin cleavable linker

2

10

noncleavable maleimidocaproyl(mc) linker

2

11

protease-cleavable linker

2

12

sortasemediated antibody conjugationtechnology(SMAC)

2

13

4APnon-cleavable linker

1

14

acid-lab ie 4-(4'-acetyl phenoxy) but an oic acid(acetyl butyrate) linker

1

15

amide bond

1

16

bifunctiona1 4-(4-acetyl phenoxy) butanoicacid(Ac But)

1

17

bioresversible linker

1

18

cathepsin B-sensitive cleavable linker

1

19

cathepsin-deavablemaleimidocaproyl-valine-alanine(MC-Val-A1a) type linker

1

20

CL2A linker

1

Stage

Toxin TOP 3

Number of pipelines

Phase 3

SPDB 1inker

2

tetrapeptide-based linker、PEG spacer、MCC

1

Phase 2

Cleavable valine-citrulline linker

4

cleavable linker

3

mc-val-cit-P ABC、non-de av able linker、peptidelinker、SPD B linker

2

Phase 1

Cleavable valine-citrulline linker

4

cleavable linker

4

SMCC

2

Preclinical

Cleavable valine-citrulline linker

4

non-cleavable linker、SMCC

3

SMAC、non-polyethylene glycol linker

2