loncastuximab tesirine

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Ligands
loncastuximab tesirine

GtoPdb Ligand ID: 11521

Synonyms: ADCT-402 | ADCT402 | loncastuximab tesirine-lpyl | RB4v1.2-SG-3249 | Zynlonta®

loncastuximab tesirine is an approved drug (FDA (2021), EMA (2022))

Compound class: Antibody

Comment: Loncastuximab tesirine (ADCT-402) is an antibody-drug conjugate that delivers the toxic payload teserine (pyrrolobenzodiazepine dimer SG3249, which acts as a DNA alkylating and cross-linking agent [3]) to CD19-expressing B cells [4].

References
1. Hamadani M, Radford J, Carlo-Stella C, Caimi PF, Reid E, O'Connor OA, Feingold JM, Ardeshna KM, Townsend W, Solh M et al.. (2021) Final results of a phase 1 study of loncastuximab tesirine in relapsed/refractory B-cell non-Hodgkin lymphoma. Blood, 137 (19): 2634-2645. [PMID:33211842]
2. Jain N, Stock W, Zeidan A, Atallah E, McCloskey J, Heffner L, Tomlinson B, Bhatnagar B, Feingold J, Ungar D et al.. (2020) Loncastuximab tesirine, an anti-CD19 antibody-drug conjugate, in relapsed/refractory B-cell acute lymphoblastic leukemia. Blood Adv, 4 (3): 449-457. [PMID:32012214]
3. Tiberghien AC, Levy JN, Masterson LA, Patel NV, Adams LR, Corbett S, Williams DG, Hartley JA, Howard PW. (2016) Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett, 7 (11): 983-987. [PMID:27882195]
4. Zammarchi F, Corbett S, Adams L, Tyrer PC, Kiakos K, Janghra N, Marafioti T, Britten CE, Havenith CEG, Chivers S et al.. (2018) ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies. Blood, 131 (10): 1094-1105. [PMID:29298756]

References

1. Hamadani M, Radford J, Carlo-Stella C, Caimi PF, Reid E, O'Connor OA, Feingold JM, Ardeshna KM, Townsend W, Solh M et al.. (2021)
Final results of a phase 1 study of loncastuximab tesirine in relapsed/refractory B-cell non-Hodgkin lymphoma.
Blood, 137 (19): 2634-2645. [PMID:33211842]

2. Jain N, Stock W, Zeidan A, Atallah E, McCloskey J, Heffner L, Tomlinson B, Bhatnagar B, Feingold J, Ungar D et al.. (2020)
Loncastuximab tesirine, an anti-CD19 antibody-drug conjugate, in relapsed/refractory B-cell acute lymphoblastic leukemia.
Blood Adv, 4 (3): 449-457. [PMID:32012214]

3. Tiberghien AC, Levy JN, Masterson LA, Patel NV, Adams LR, Corbett S, Williams DG, Hartley JA, Howard PW. (2016)
Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload.
ACS Med Chem Lett, 7 (11): 983-987. [PMID:27882195]

4. Zammarchi F, Corbett S, Adams L, Tyrer PC, Kiakos K, Janghra N, Marafioti T, Britten CE, Havenith CEG, Chivers S et al.. (2018)
ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies.
Blood, 131 (10): 1094-1105. [PMID:29298756]