OXERVATE
Clinical safety rating: caution
Comprehensive 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 |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OXERVATE (OXERVATE).
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or milk production. Caution advised; M/P ratio unknown. |
| 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 |
■ 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 becaplermin or any product component; active neoplasm at the application site; patients with a history of malignancy (relative contraindication based on black box warning).
| 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. |
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| No specific maternal or fetal monitoring required beyond routine pregnancy care. |
| Fertility Effects | No data on fertility effects in humans. Animal studies not conducted. |