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Ilevro

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Ilevro

CLINICAL PHARMACOLOGY

Mechanism of Action

After topical ocular dosing, nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a nonsteroidal anti-inflammatory drug. Nepafenac and amfenac are thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production.

Pharmacokinetics

Following bilateral topical ocular once-daily dosing of ILEVRO™ (nepafenac ophthalmic suspension), 0.3%, the concentrations of nepafenac and amfenac peaked at a median time of 0.5 hour and 0.75 hour, respectively on both Day 1 and Day 4. The mean steady-state Cmax for nepafenac and for amfenac were 0.847 ± 0.269 ng/mL and 1.13 ± 0.491 ng/mL, respectively.

Nepafenac at concentrations up to 3000 ng/mL and amfenac at concentrations up to 1000 ng/mL did not inhibit the in vitro metabolism of 6 specific marker substrates of cytochrome P450 (CYP) isozymes (CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4). Therefore, drug-drug interactions involving CYP mediated metabolism of concomitantly administered drugs are unlikely.

Clinical Studies

In two double masked, randomized clinical trials in which patients were dosed daily beginning one day prior to cataract surgery, continued on the day of surgery and for the first two weeks of the postoperative period, ILEVRO™ (nepafenac ophthalmic suspension), 0.3% demonstrated superior clinical efficacy compared to its vehicle in treating postoperative pain and inflammation.

Treatment effect over vehicle for resolution of ocular pain occurred as early as day 1 post-surgery. Treatment effect over vehicle for resolution of inflammation was significantly better than vehicle in both studies at day 7 and day 14 post-surgery.

Inflammation and Ocular Pain Resolution Results of Nepafenac ophthalmic suspension, 0.3% versus Vehicle at Day 14 Post-surgery (All-Randomized Population)

Studies Treatment Inflammation Resolution at Postop Day 14 Ocular Pain Resolution at Postop Day 14
Study 1 Nepafenac ophthalmic suspension, 0.3% (n/N)1 552/851 (65%) 734/851 (86%)
NEVANAC (n/N)1 568/845 (67%) 737/845 (87%)
Vehicle (n/N)1 67/211 (32%) 98/211 (46%)
Difference (95% CI) 2 33% (26%, 40%) 40% (32%, 47%)
Study 2 Nepafenac ophthalmic suspension, 0.3% (n/N)1 331/540 (61%) 456/540 (84%)
Vehicle (n/N)1 63/268 (24%) 101/268 (38%)
Difference (95% CI)2 38% (31%, 45%) 47% (40%, 54%)
1n/N is the ratio of those with complete resolution of anterior chamber cell and flare by the postoperative day 14 visit over all randomized subjects.
2Difference is (Nepafenac ophthalmic suspension, 0.3% – vehicle). The 95% confidence interval is derived using asymptotic approximation.

Last reviewed on RxList: 1/4/2013
This monograph has been modified to include the generic and brand name in many instances.

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