OXERVATE
Clinical safety rating
cautionComprehensive clinical and safety monograph for OXERVATE (OXERVATE).
OXERVATE (becaplermin) is a recombinant human platelet-derived growth factor (rhPDGF-BB) that promotes wound healing by stimulating chemotaxis and mitogenesis of fibroblasts, smooth muscle cells, and other cells involved in tissue repair.
| Metabolism | Becaplermin is a protein that is expected to be degraded into small peptides and amino acids via general protein catabolism; specific hepatic metabolism is not a significant pathway. |
| Excretion | Primarily renal elimination of the active metabolite (Cenegermin) as small peptides and amino acids; unchanged drug excretion is negligible |
| Half-life | Terminal elimination half-life of Cenegermin is approximately 12 hours following topical ocular administration, supporting once-daily dosing |
| Protein binding | Cenegermin binding to plasma proteins is minimal (<10%) due to its small protein nature |
| Volume of Distribution | Vd not determined for topical ocular route; systemic exposure is low, with Vd estimated less than 0.1 L/kg based on limited systemic absorption |
| Bioavailability | Topical ocular: Systemic bioavailability is negligible (<1%) due to low corneal penetration and extensive proteolysis at the ocular surface |
| Onset of Action | Topical: Clinical improvement in corneal healing (e.g., reduction in defect size) observed within 2–4 weeks of daily dosing |
| Duration of Action | Sustained corneal re-epithelialization over the 8-week treatment course; effects may persist after discontinuation |
| Molecular Weight | 66.5 |
1 drop in the affected eye(s) twice daily, approximately 6 hours apart.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. |
| Geriatric use | No specific dose adjustment required; use same dosing as adults. |
| 1st trimester | No adequate and well-controlled studies in pregnant women; animal studies have not been conducted. Risk cannot be ruled out. |
| 2nd trimester | No adequate and well-controlled studies in pregnant women; animal studies have not been conducted. Risk cannot be ruled out. |
| 3rd trimester | No adequate and well-controlled studies in pregnant women; animal studies have not been conducted. Risk cannot be ruled out. |
Clinical note
Comprehensive clinical and safety monograph for OXERVATE (OXERVATE).
| Placental transfer | Unknown; molecular weight suggests potential for placental transfer, but no data available. |
| Breastfeeding | Unknown if distributed in human milk; caution advised due to lack of data. |
| Lactation Rating | L3 (Limited Data) |
| Teratogenic Risk | OXERVATE contains cenegermin, a recombinant human nerve growth factor. No adequate and well-controlled studies in pregnant women. Animal reproductive studies have not been conducted. Risk cannot be ruled out; use only if potential benefit justifies potential risk to fetus. First trimester: unknown risk; second and third trimesters: unknown risk. |
| Fetal Monitoring | No specific maternal or fetal monitoring required beyond routine pregnancy care. |
| Fertility Effects | No data on fertility effects in humans. Animal studies not conducted. |
■ FDA Black Box Warning
OXERVATE has been associated with an increased risk of mortality from secondary malignancies in patients who have had a malignant neoplasm. The drug should not be used in patients with active malignancy.
| Serious Effects |
Known hypersensitivity to cenegermin or any excipients
| Precautions | Increased risk of malignancy in patients with a history of malignancy; application to ulcers with malignant cells may promote tumor growth; use only on clean, non-infected ulcers; monitor for signs of infection; avoid application to wounds with exposed bone, tendon, or joint capsule. |
| Food/Dietary | None known; no significant food interactions reported. |
| Clinical Pearls | OXERVATE (cenegermin-bkbj) is a recombinant human nerve growth factor for neurotrophic keratitis. Administer as one drop in the affected eye(s) six times daily at 2-hour intervals for 8 weeks. Refrigerate at 2-8°C; do not freeze. Protect from light. Discard unused drops after 1 week of first opening. Monitor for corneal epithelial defect closure. Use with caution in patients with active ocular infections or inflammation. |
| Patient Advice | Wash hands before each use. · Instill one drop in the affected eye(s) every 2 hours, 6 times daily. · Refrigerate the medication at all times; do not freeze. · Use within 1 week after opening the vial. · Avoid touching the dropper tip to any surface. · Do not use contact lenses during treatment. · Report any eye pain, redness, or vision changes immediately. · Complete the full 8-week course even if symptoms improve. |
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