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. 2022 Jan 22;25:101300. doi: 10.1016/j.ajoc.2022.101300

Table 1.

Summary of small molecule kinase inhibitors and their ocular toxicities.2,3,9, 10, 11, 12, 13,27

Name Known Target Indications Ocular toxicity
Anaplastic lymphoma kinase (ALK)
Alectinib ALK and RET ALK + NSCLC Nil
Brigatinib ALK, ROS1, IGF-1R, Flt3, EGFR ALK + NSCLC after crizotinib Nil
Ceritinib ALK, IGF-1R, InsR, ROS1 ALK + NSCLC as first-line treatment or after crizotinib resistance Nonspecitic vision disorder (vision impairment, blurred vision, photopsia, accommodation disorder)
Crizotinib ALK, c-Met (HGFR), ROS1, MST1R ALK+, ROS1+ NSCLC Nonspecific vision disorder (diplopia, photopsia, photophobia, blurred vision, visual field defect, floaters)
Entrectinib TRKA/B/C, ROS1, ALK ROS1+ NSCLC; solid tumors with NTRK fusion proteins Nil
Lorlatinib ALK ALK + NSCLC Nil
Bosutinib BCR-ABL, Src, Lyn, Hck CML Nil
Dasatinib BCR-ABL, EGFR, Src, Lck, Yes, Fyn, Kit, EphA2, PDGFRβ Ph + chronic ML and ALL Optic neuropathy
VKH like illness
Dry eye/conjunctivitis
Blurred vision
Periorbital oedema
Imatinib BCR-ABL, Kit, PDGFR Ph + CML or ALL, CEL, DFSP, HES, GIST, MDS/MDP VKH-like illness
Glaucoma
Neovascularisation, retinal haemorrhage, macular oedema
Optic neuropathy/papilloedema
Periorbital/eyelid oedema
Keratitis/conjunctivitis/blepharitis
Scleral/conjunctival haemorrhage
Cataract
Nilotinib BCR-ABL, PDGFR, DDR1 Ph + CLL Iridocyclitis
Periorbital oedema
Dry eye
Conjunctivitis/blepharitis
Conjunctival haemorrhage/hyperaemia
Papilloedema
Ponatinib BCR-ABL, BCR-ABL T315I, VEGFR, PDGFR, FGFR, EphR, Src family kinases, Kit, RET, Tie2, Flt3 Ph + CML or ALL Nil
Epidermal growth factor receptor (EGFR)
Afatinib EGFR, ErbB2, ErbB4 NSCLC Conjunctivitis
Keratitis
Dacomitinib EGFR/ErbB2/ErbB4 EGFR- mutated NSCLC Nil
Erlotinib EGFR SCLC and PaC Ocular toxoplasmosis
Trichomegaly and eyelid disease
Corneal erosion and ocular surface disease (conjunctivitis/keratitis)
Corneal perforation
Gefitinib EGFR NCLC Trichomegaly and eyelid disease
Corneal erosion and ocular surface disease (conjunctivitis)
Corneal perforation
Ocular ischaemia/haemorrhage
Uveitis
Lapatinib EGFR, ErbB2 BC Nil
Neratinib ErbB2/HER2 HER2+ breast cancer Nil
Osimertinib EGFR T970 M NSCLC Nil
Vandetanib EGFRs, VEGFRs, RET, Brk, Tie2, EphRs, Src family kinases MTC Verticillata
Conjunctivitis
Corneal structural change
Glaucoma
Cataract
FMS-like tyrosine kinase 3 (FLT3)
Gilteritinib FLT3 AMLwith FLT3 mutation5 Nil
Midostaurin FLT3 ALL Flt3 mutation+ Nil
Erdafitinib FGFR1/2/3/4 Urothelial carcinoma Dry eye
Blurred vision
RPE detachment
Retinal detachment
Ruxolitinib JAK1 and 2 MF and PV Nil
Larotrectinib NTRK Solid tumors with NTRK gene fusion proteins Nil
Axitinib VEGFR1/2/3, PDGFRβ RCC Retinal artery/vein occlusion
Carbozantinib RET, Met, VEGFR1/2/3, Kit, TrkB, Flt3, Axl, Tie2, ROS1 Metastatic MTC, advanced RCC and HCC Nil
Lenvatinib VEGFRs, FGFRs, PDGFR, Kit, RET DTC Nil
Pazopanib VEGFR1/2/3, PDGFRα/β, FGFR1/3, Kit, Lck, Fms, Itk RCC, STS Ocular surface
Lid changes
Retinal detachment
Regorafenib VEGFR1/2/3, BCR-ABL, BRAF, BRAF(V600E), Kit, PDGFRα/β, RET, FGFR1/2, Tie2, Eph2A CRC, GIST Nil
Sorafenib B/C-Raf, BRAF (V600E), Kit, Flt3, RET, VEGFR1/2/3, PDGFRβ RCC, DTC and HCC Ocular surface
Lid changes
Retinal detachment
Sunitinib PDGFRα/β, VEGFR1/2/3, Kit, Flt3, CSF-1R, RET RCC, GIST, PNET Ocular surface
Lid changes (periorbital oedema)
Retinal detachment
Dabrafenib BRAF Melanoma and NSCLC with BRAF mutations Photosensitivity
VKH like illness
RPE changes and subretinal fluid
Uveitis
Retinal vein occlusion
Encorafenib BRAFV600E/K BRAFV600E/K mutant melanoma with binimetinib Nil
Vemurafenib A/B/C-Raf, BRAF (V600E), SRMS, ACK1, MAP4K5, FGR Melanoma with BRAFV600E mutation and ECD Uveitis
Conjunctivitis and dry eye
CMORPE changes and RPE detachment
Retinal vein occlusion
Central serous retinopathy
TK inhibitors
Acalabrutinib Bruton tyrosine kinase MCL Nil
Ibrutinib Bruton tyrosine kinase MCL, CLL, WM, graph vs host disease. Visual disturbance
Cataract
Dry eye
Subconjunctival haemorrhage
Branch retinal artery occlusion
Cystoid macular oedema
MEK inhibitors
Binimetinib MEK1/2 BRAF V600E/K melanoma with encorafenib Chorioretinopathy
Photopsia/visual impairment
Retinal detachment
Macular oedema
Retinopathy
Visual impairment
Cobimetinib MEK1/2 Melanoma with BRAF V600E/K mutations with vemurafenib Uveitis
CMORPE changes and RPE detachment
Trametinib MEK1/2 Melanoma (2013) and NSCLC (2017) with BRAF mutations VKH-like illness
RPE changes and subretinal fluid Uveitis
Retinal vein occlusion
Central serous retinopathy
Periorbital oedema
Dry eye
Abemaciclib CDK4/6 HR+, HER– BC Nil
Palbociclib CDK4/6 ER+ and HER2– BC Nil
Ribociclib CDK4/6 HR + -EGFR– metastatic BC Nil