Table 1. The listing of Antibody-drug conjugates(ADCs) Approved by FDA (upto 2024):
ADC Drug | Trade name | Maker | Disease Indication | Payload/Payload Class | Payload Action | Target | mAb | Linker | DAR | Approval Year |
Mirvetuximab soravtansine | ELAHERE | ImmunoGen | Platinum-Resistant Ovarian Cancer | Maytansinoid DM4 | Folate receptor alpha | FRα | IgG1 | / | N/A | 2022 (Expanded use 2023) |
Tisotumab vedotin-tftv | Tivdak | Seagen Inc | Recurrent or metastatic cervical cancer | MMAE/auristatin | microtubule inhibitor | Tissue factor | IgG1 | enzyme cleavable | 4 | 2021 |
Loncastuximab tesirine-lpyl | Zynlonta | ADC Therapeutics | Large B-cell lymphoma | SG3199/PBD dimer | DNA cleavage | CD19 | IgG1 | enzyme cleavable | SG3199/PBD dimer | 2021 |
Belantamab mafodotin-blmf | Blenrep | GlaxoSmithKline (GSK) | adult patients with relapsed or refractory multiple myeloma | MMAF/auristatin | microtubule inhibitor | BCMA | IgG1 | non-cleavable | 4 | 2020, withdrawn on 22 Nov. 2022 |
Sacituzumab govitecan | Trodelvy | Immunomedics | adult patients with metastatic triple-negative breast cancer (mTNBC) who have received at least two prior therapies for patients with relapsed or refractory metastatic disease | SN-38/camptothecin | TOP1 inhibitor | TROP2 | IgG1 | acid cleavable | 7.6 | 2020 |
Trastuzumab deruxtecan | Enhertu | AstraZeneca/Daiichi Sankyo | adult patients with unresectable or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2 based regimens | DXd/camptothecin | TOP1 inhibitor | HER2 | IgG1 | enzyme cleavable | 8 | 2019 |
Enfortumab vedotin | Padcev | Astellas/Seagen Genetics | adult patients with locally advanced or metastatic urothelial cancer who have received a PD-1 or PD-L1 inhibitor, and a Pt-containing therapy | MMAE/auristatin | microtubule inhibitor | Nectin4 | IgG1 | enzyme cleavable | 3.8 | 2019 |
Polatuzumab vedotin-piiq | Polivy | Genentech, Roche | relapsed or refractory (R/R) diffuse large B-cell lymphoma (DLBCL) | MMAE/auristatin | microtubule inhibitor | CD79 | IgG1 | enzyme cleavable | 3.5 | 2019 |
Moxetumomab pasudotox | Lumoxiti | Astrazeneca | adults with relapsed or refractory hairy cell leukemia (HCL) | PE38 (Pseudotox) | / | CD22 | IgG1 | Cleavable | N/A | 2018 |
Inotuzumab ozogamicin | Besponsa | Pfizer/Wyeth | relapsed or refractory CD22-positive B-cell precursor acute lymphoblastic leukemia | ozogamicin/calicheamicin | DNA cleavage | CD22 | IgG4 | acid cleavable | 6 | 2017 |
Trastuzumab emtansine | Kadcyla | Genentech, Roche | HER2-positive metastatic breast cancer (mBC) following treatment with trastuzumab and a maytansinoid | DM1/maytansinoid | microtubule inhibitor | HER2 | IgG1 | non-cleavable | 3.5 | 2013 |
Brentuximab vedotin | Adcetris | Seagen Genetics, Millennium/Takeda | relapsed HL and relapsed sALCL | MMAE/auristatin | microtubule inhibitor | CD30 | IgG1 | enzyme cleavable | 4 | 2011 |
Gemtuzumab ozogamicin | Mylotarg | Pfizer/Wyeth | relapsed acute myelogenous leukemia (AML) | ozogamicin/calicheamicin | DNA cleavage | CD33 | IgG4 | acid cleavable | 2–3 | 2017; 2000 |
A stable link between the antibody and the cytotoxic agent is key to ADC conjugation. A strong ADC linker ensures that less of the cytotoxic payload is lost in circulation, improving safety. It also delivers more of the drug to the cancer cell, increasing efficacy. Linkers use chemical motifs like disulfides, hydrazones, peptides (cleavable), or thioethers (non-cleavable) to control drug delivery.
AxisPharm develops a wide range of linkers and offers custom linker synthesis. Our catalog includes click chemistry tools (DBCO, Tetrazine, TCO, BCN, Cyclopropene), biotin, PEG, peptide, glucuronide, and photo-cleavable linkers. We also offer fluorescent dye probes and folic acid PEG linkers.
As a customer-focused contract research company, we provide flexible ADC linker kits and bioconjugation services at competitive prices.
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