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. Author manuscript; available in PMC: 2024 Jun 1.
Published in final edited form as: Curr Ophthalmol Rep. 2024 Mar 24;12(2):13–22. doi: 10.1007/s40135-024-00322-5

Table 1.

Ocular Surface Toxicities in FDA-Approved Antibody–Drug-Conjugates (ADCs)

Drug Name Indication Antibody (Ocular Surface Expression) Payload (Mechanism) Prevalence of corneal pseudomicrocysts Other Ocular Surface AEs Ocular Surface Preventive Therapies Efficacy of Ocular Surface Preventive Therapies References
Belantamab mafodotin (Blenrep)* Relapsed or refractory multiple myeloma BCMA (Not expressed) MMAF (Microtubule disruption) 68–78%

  • Keratopathy (76%)

  • Dry eye (19%)

  • Prednisolone phosphate 1 % or Dexamethasone 0.1 % eye drops 4x/day for 4–7 days starting 1 day before each infusion

  • Preservative-free artificial tears (PF-ATs) 4x/day from start of infusion

  • Topical steroids had no effect on preventing corneal changes

 [17••, 23, 26, 30, 33, 44–46]
Mirvetuximab soravtansine (Elahere) Epithelial ovarian, fallopian tube, or primary peritoneal cancer FRα (Conjunctiva) DM4 (Microtubule disruption) 41–100%

  • Keratopathy (29%)

  • Dry eye (25%)

  • Prednisolone acetate 1 % eye drops 4–6x/day for 10 days after infusion

  • FJuoromethoJone acetate (FML) eye drops tapered over 4–6 weeks

  • PF-ATs daily

  • FML for 4–6 weeks cleared corneal pseudomicrocysts and recovered visual acuity

  • Prednisolone acetate reduced rate of keratopathy from 41 to 30%

 [28,33,38,46,47]
Trastuzumab emtansine (Kadcyla) HER2 + breast cancer HER2 (Cornea & conjunctiva) DM1 (Microtubule disruption) 100%

  • Dry eye (10%)

  • Conjunctivitis (4%)

 Not reported Not reported [33, 46, 48, 49]
Tisotumab vedotin (Tivdak) Recurrent or metastatic cervical cancer Tissue factor (Cornea & conjunctiva) MMAE (Microtubule disruption) Not reported

  • Conjunctivitis (43%)

  • Conjunctival AEs (40%)

  • Dry eye (23%)

  • Corneal AEs (21%)

  • Keratitis (11%)

  • Dexamethasone 0.1 % eye drops prior to infusion and 3x/day for 3 days after infusion

  • Brimonidine tartrate 0.2% eye drops 3 times 10 min prior to infusion

  • PF-ATs as needed until 30 days after last infusion

  • Cold eye masks over each eye during infusion

  • In an ocular substudy, preventive therapeutic regimen reduced rate of conjunctivitis from 80 to 28% and rate of all ocular AEs from 80 to 60%

 [14•, 33, 46, 50–52]
Enfortumab vedotin (Padcev) Urothelial bladder cancer Nectin4 (Cornea & conjunctiva) MMAE (Microtubule disruption) Not reported

  • Dry eye (36%)

  • PF-ATs as needed

  • Topical steroids (dosage and frequency not specified)

 Not reported [8, 33, 46, 53]
Trastuzumab deruxtecan (Enhertu) HER2 + breast cancer HER2 (Cornea & conjunctiva) Camptothecin (DNA damage) Not reported

  • Dry eye (11%)

 Not reported Not reported [33, 46, 54, 55]
Gemtuzumab ozogamicin (Mylotarg) Newly diagnosed, relapsed, or refractory acute myeloid leukemia CD33 (Conjunctiva) Calicheamicin (DNA damage) NA NA NA NA [33, 46, 56]
Brentuximab vedotin (Adcetris) Lymphoma CD30 (Not expressed) MMAE (Microtubule disruption) NA NA NA NA [33, 46, 57]
Inotuzumab ozogamicin (Besponsa) Relapsed or refractory B cell acute lymphoblastic leukemia CD22 (Conjunctiva) Calicheamicin (DNA damage) NA NA NA NA [33, 46, 58]
Polatuzumab vedotin (Polivy) Relapsed or refractory diffuse large B cell lymphoma CD79b (Conjunctiva) MMAE (Microtubule disruption) NA NA NA NA [33, 46, 59]
Sacituzumab govitecan (Trodelvy) Metastatic triplenegative breast cancer; urothelial bladder cancer TROP2 (Cornea & conjunctiva) Camptothecin (DNA damage) NA NA NA NA [33, 46, 60]
Loncastuximab tesirine (Zynlonta) Large B cell lymphoma CD19 (Cornea) PBD dimer (DNA damage) NA NA NA NA (33, 46, 61)
*

Withdrawn from US market after failure to meet FDA requirements from DREAMM-3 phase III confirmatory trial