July 2019
Volume 60, Issue 9
Open Access
ARVO Annual Meeting Abstract  |   July 2019
A novel nintedanib ophthalmic nanosuspension (AG-86893) for the treatment of pterygium
Author Affiliations & Notes
  • Tan Nguyen
    Allgenesis Biotherapeutics Inc., Taipei, Taiwan
  • Sandy Lai
    Allgenesis Biotherapeutics Inc., Taipei, Taiwan
  • Thomas Malone
    TCM Consulting, Irvine, California, United States
  • Larry A Wheeler
    Zeteo Discovery Research LLC, Irvine, California, United States
  • Madhu Cherukury
    Allgenesis Biotherapeutics Inc., Taipei, Taiwan
  • Footnotes
    Commercial Relationships   Tan Nguyen, Allgenesis Biotherapeutics Inc. (E), Allgenesis Biotherapeutics Inc. (P); Sandy Lai, Allgenesis Biotherapeutics Inc. (E), Allgenesis Biotherapeutics Inc. (P); Thomas Malone, TCM Consulting (C); Larry Wheeler, Zeteo Discovery Research LLC (C); Madhu Cherukury, Allgenesis Biotherapeutics Inc. (E), Allgenesis Biotherapeutics Inc. (S)
  • Footnotes
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Investigative Ophthalmology & Visual Science July 2019, Vol.60, 2094. doi:
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      Tan Nguyen, Sandy Lai, Thomas Malone, Larry A Wheeler, Madhu Cherukury; A novel nintedanib ophthalmic nanosuspension (AG-86893) for the treatment of pterygium. Invest. Ophthalmol. Vis. Sci. 2019;60(9):2094.

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      © ARVO (1962-2015); The Authors (2016-present)

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Purpose : Cytokines such as epidermal growth factor, fibroblast growth factor-2, nerve growth factor, platelet derived growth factor, transforming growth factor-β and vascular endothelial growth factor are thought to play a role in the formation of pterygium. We hypothesized that inhibition of one or more of these cytokines by tyrosine kinase inhibitors (TKIs) could be used to treat pterygium. We tested our hypothesis using a rabbit corneal neovascularization model.

Methods : Microsuspensions (0.3%) of three TKIs (nintedanib, axitinib, and sorafenib) were tested in a rabbit corneal neovascularization (NV) model to determine their ability to inhibit NV following three times daily (TID) ocular dosing for 14 days (N=6 eyes/group). AG-86893 (0.1 – 1%) was developed and tested to assess its efficacy following TID dosing for 7 days after induction of NV. Furthermore, the ocular pharmacokinetics of AG-86893 (0.1%) in rabbits were determined after a single topical eye drop (N = 4 eyes/group) and compared to that of a solution formulation (0.1%). Pharmacokinetic parameters (Cmax, Tmax, AUC, T1/2, where applicable), were determined in key ocular tissues using Phoenix WinNonLin v. 7.0.

Results : Of the TKIs tested, nintedanib and axitinib showed significant inhibition on blood vessel growth, blood vessel length, and area of NV on day 7 compared to vehicle (p<0.0001). Surprisingly, sorafenib had little effect. AG-86893 equally inhibited NV at all 3 doses tested, indicating that the maximal inhibitory effect was reached at 0.1% TID. All 3 doses showed significant inhibition compared to vehicle (p<0.0006). AG-86893 showed higher exposure and longer ocular tissue half-lives compared to a solution formulation.

Conclusions : Our results show that TKIs have the potential to treat pterygium. AG-86893 has potential for treating pterygium with once daily ocular dosing.

This abstract was presented at the 2019 ARVO Annual Meeting, held in Vancouver, Canada, April 28 - May 2, 2019.


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