Global Oncology Trends 2024: Outlook to 2028: IQVia; 2024.

Masters JC, Nickens DJ, Xuan D, Shazer RL, Amantea M. Clinical toxicity of antibody drug conjugates: a meta-analysis of payloads. Invest New Drugs. 2018;36(1):121–35.

Article  CAS  PubMed  Google Scholar 

Donaghy H. Effects of antibody, drug and linker on the preclinical and clinical toxicities of antibody-drug conjugates. MAbs. 2016;8(4):659–71.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Yu X, Li W, Huang W, Xiao B, Long J, Wang Q, et al. Simultaneous quantification of total antibody and conjugated payload for DS001 in rat serum using a hybrid immuno-capture LC-MS/MS. AAPS J. 2025;27(1):23.

Article  CAS  PubMed  Google Scholar 

Mahmood I. Clinical pharmacology of antibody-drug conjugates. Antibodies (Basel). 2021;10(2):20.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Colombo R, Rich JR. The therapeutic window of antibody drug conjugates: a dogma in need of revision. Cancer Cell. 2022;40(11):1255–63.

Article  CAS  PubMed  Google Scholar 

Zuo P. Capturing the magic bullet: pharmacokinetic principles and modeling of antibody-drug conjugates. Aaps j. 2020;22(5):105.

Article  CAS  PubMed  Google Scholar 

US Food Drug Administration. Clinical pharmacology considerations for antibody-drug conjugates guidance for industry: guidance for industry. 2024.

Géraud A, Gougis P, de Nonneville A, Beaufils M, Bertucci F, Billon E, et al. Pharmacology and pharmacokinetics of antibody-drug conjugates, where do we stand? Cancer Treat Rev. 2025;135:102922.

Article  PubMed  Google Scholar 

ASReview. ASReview: Open Source systematic review software with machine learning. [cited]. https://asreview.nl/.

Van De Schoot R, De Bruin J, Schram R, Zahedi P, De Boer J, Weijdema F, et al. An open source machine learning framework for efficient and transparent systematic reviews. Nat Mach Intell. 2021;3(2):125–33.

Article  Google Scholar 

Boetje J, van de Schoot R. The SAFE procedure: a practical stopping heuristic for active learning-based screening in systematic reviews and meta-analyses. Syst Rev. 2024;13(1):81.

Article  PubMed  PubMed Central  Google Scholar 

Krop IE, Beeram M, Modi S, Jones SF, Holden SN, Yu W, et al. Phase I study of trastuzumab-DM1, an HER2 antibody-drug conjugate, given every 3 weeks to patients with HER2-positive metastatic breast cancer. J Clin Oncol. 2010;28(16):2698–704.

Article  CAS  PubMed  Google Scholar 

Girish S, Gupta M, Wang B, Lu D, Krop IE, Vogel CL, et al. Clinical pharmacology of trastuzumab emtansine (T-DM1): an antibody-drug conjugate in development for the treatment of HER2-positive cancer. Cancer Chemother Pharmacol. 2012;69(5):1229–40.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Food and Drug Administration: Center for Drug Evaluation Research. Clinical pharmacology and biopharmaceutics review KADCYLA (trastuzumab emtansine). 2012.

Li C, Wang B, Chen SC, Wada R, Lu D, Wang X, et al. Exposure-response analyses of trastuzumab emtansine in patients with HER2-positive advanced breast cancer previously treated with trastuzumab and a taxane. Cancer Chemother Pharmacol. 2017;80(6):1079–90.

Article  CAS  PubMed  Google Scholar 

Chen SC, Quartino A, Polhamus D, Riggs M, French J, Wang X, et al. Population pharmacokinetics and exposure-response of trastuzumab emtansine in advanced breast cancer previously treated with ≥2 HER2-targeted regimens. Br J Clin Pharmacol. 2017;83(12):2767–77.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Wang J, Song P, Schrieber S, Liu Q, Xu Q, Blumenthal G, et al. Exposure–response relationship of T-DM1: insight into dose optimization for patients with HER2-positive metastatic breast cancer. Clin Pharmacol Ther. 2014;95(5):558–64.

Article  CAS  PubMed  Google Scholar 

Yoshihara K, Kobayashi Y, Endo S, Fukae M, Hennig S, Kastrissios H, et al. Trastuzumab deruxtecan dosing in human epidermal growth factor receptor 2-positive gastric cancer: population pharmacokinetic modeling and exposure-response analysis. J Clin Pharmacol. 2023;63(11):1232–43.

Article  CAS  PubMed  Google Scholar 

Yin O, Xiong Y, Endo S, Yoshihara K, Garimella T, AbuTarif M, et al. Population pharmacokinetics of trastuzumab deruxtecan in patients with HER2-positive breast cancer and other solid tumors. Clin Pharmacol Ther. 2021;109(5):1314–25.

Article  CAS  PubMed  Google Scholar 

Food and Drug Administration: Center for Drug Evaluation Research. NDA/BLA multi-disciplinary review and evaluation ENHERTU (fam-trastuzumab deruxtecan-nxki). 2019.

Yin O, Iwata H, Lin CC, Tamura K, Watanabe J, Wada R, et al. Exposure-response relationships in patients with HER2-positive metastatic breast cancer and other solid tumors treated with trastuzumab deruxtecan. Clin Pharmacol Ther. 2021;110(4):986–96.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Food and Drug Administration: Center for Drug Evaluation Research. NDA/BLA multi-disciplinary review and evaluation PADCEV (enfortumab vedotin-ievx). 2019.

Zuo P, Bonate P, Garg A, Matsangou M, Tang M. Population pharmacokinetic modeling and exposure-response analysis for the antibody-drug conjugate enfortumab vedotin in locally advanced or metastatic urothelial carcinoma. Clin Pharmacol Ther. 2024;116(5):1278–88.

Article  CAS  PubMed  Google Scholar 

Tang M, Garg A, Bonate PL, Rosenberg JE, Matsangou M, Kadokura T, et al. Clinical pharmacology of the antibody-drug conjugate enfortumab vedotin in advanced urothelial carcinoma and other malignant solid tumors. Clin Pharmacokinet. 2024;63(4):423–38.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Sathe AG, Singh I, Singh P, Diderichsen PM, Wang X, Chang P, et al. Population pharmacokinetics of sacituzumab govitecan in patients with metastatic triple-negative breast cancer and other solid tumors. Clin Pharmacokinet. 2024;63(5):669–81.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Food and Drug Administration: Center for Drug Evaluation Research. BLA multi-disciplinary review and evaluation TRODELVY (sacituzumab govitecan). 2019.

Sathe AG, Diderichsen PM, Fauchet F, Phan SC, Girish S, Othman AA. Exposure-response analyses of sacituzumab govitecan efficacy and safety in patients with metastatic triple-negative breast cancer. Clin Pharmacol Ther. 2025;117(2):570–8.

Article  CAS  PubMed  Google Scholar 

Gilead Sciences I. Trodelvy® (sacituzumab govitecan-hziy) Pharmacokinetics 2023 [cited 2025 6th August ]; 2024. https://www.askgileadmedical.com/docs/trodelvy/trodelvy-pharmacokinetics.

Tu YP, Hanze E, Zhu F, Lagraauw HM, Sloss CM, Method M, et al. Population pharmacokinetics of mirvetuximab soravtansine in patients with folate receptor-α positive ovarian cancer: the antibody-drug conjugate, payload and metabolite. Br J Clin Pharmacol. 2024;90(2):568–81.

Article  CAS  PubMed  Google Scholar 

Food and Drug Administration: Center for Drug Evaluation Research. NDA/BLA multi-disciplinary review and evaluation ELAHERE (mirvetuximab soravtansine-gynx). 2022.

Tu YP, Lagraauw HM, Method M, Wang Y, Hanze E, Li L, et al. Exposure-response relationships of mirvetuximab soravtansine in patients with folate receptor-α-positive ovarian cancer: Justification of therapeutic dose regimen. Br J Clin Pharmacol. 2025;91(1):220–31.

Article  CAS  PubMed  Google Scholar 

Gibiansky L, Passey C, Voellinger J, Gunawan R, Hanley WD, Gupta M, et al. Population pharmacokinetic analysis for tisotumab vedotin in patients with locally advanced and/or metastatic solid tumors. CPT Pharmacometr Syst Pharmacol. 2022;11(10):1358–70.

Article  CAS  Google Scholar 

Passey C, Voellinger J, Gibiansky L, Gunawan R, Nicacio L, Soumaoro I, et al. Exposure-safety and exposure-efficacy analyses for tisotumab vedotin for patients with locally advanced or metastatic solid tumors. CPT Pharmacometr Syst Pharmacol. 2023;12(9):1262–73.

Article  CAS  Google Scholar 

European Medicines Agency Committee for Medicinal Products for Human Use (CHMP). Assessment Report Kadcyla European Medicines Agency; 2013.

European Medicines Agency Committee for Medicinal Products for Human Use (CHMP). Assessment Report Enhertu European Medicines Agency; 2020.

European Medicines Agency Committee for Medicinal Products for Human Use (CHMP). Assessment Report Padcev: European Medicines Agency; 2022.

European Medicines Agency Committee for Medicinal Products For Human Use (CHMP). Assessment Report Trodelvy; 2021.

European Medicines Agency Committee for Medicinal Products for Human Use (CHMP). Assessment Report Elahere: European Medicines Agency; 2024

Food and Drug Administration: Center for Drug Evaluation Research. NDA/BLA Multi-disciplinary Review and Evaluation TIVDAK (tisotumab-vedotin-tftv): Food and Drug Administration; 2021.

European Medicines Agency Committee for Medicinal Products for Human Use (CHMP). Assessment Report Tivdak: European Medicines Agency; 2025.

Gilead Sciences Inc. Trodelvy® (sacituzumab govitecan-hziy) Pharmacokinetics 2024 [cited 14 March 2025]. https://www.askgileadmedical.com/docs/trodelvy/trodelvy-pharmacokinetics.

Xu K, Liu L, Dere R, Mai E, Erickson R, Hendricks A, et al. Characterization of the drug-to-antibody ratio distribution for antibody–drug conjugates in plasma/serum. Bioanalysis. 2013;5(9):1057–71.

Article  CAS  PubMed  Google Scholar 

Nadkarni DV, Lee J, Jiang Q, Patel V, Sriskanda V, Dutta K, et al. Impact of drug conjugation and loading on target antigen binding and cytotoxicity in cysteine antibody-drug conjugates. Mol Pharm. 2021;18(3):889–97.

Article