REGRANEX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REGRANEX (REGRANEX).
Recombinant human platelet-derived growth factor (rhPDGF-BB) that promotes chemotaxis and proliferation of fibroblasts, smooth muscle cells, and other cells involved in wound healing, and stimulates granulation tissue formation.
| Metabolism | Metabolized locally; no systemic metabolism expected due to topical administration and minimal absorption. If absorbed, degraded by proteolytic enzymes at the wound site. |
| Excretion | Primarily renal; minimal biliary/fecal. Becaplermin is cleared renally (>90% as metabolites) with <2% excreted unchanged. Fecal elimination accounts for <10%. |
| Half-life | Terminal half-life ~30-60 minutes after topical application; prolonged in renal impairment (up to 2-3 hours). Clinical context: Short systemic exposure limits off-target effects. |
| Protein binding | ~25% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Vd ~12 L (~0.17 L/kg assuming 70 kg), indicating limited extravascular distribution due to molecular size. |
| Bioavailability | Topical: Negligible systemic bioavailability (<1% of applied dose absorbed; increased with large wounds or impaired skin barrier). |
| Onset of Action | Topical: Clinical effect (granulation tissue formation) observed within 2-4 weeks of continuous daily application. |
| Duration of Action | Duration of clinical effect is sustained with continued application; after discontinuation, wound healing progress may slow. Systemic levels decline within hours. |
Apply topically once daily, a thin layer to the full area of the ulcer, using a measured amount of gel based on ulcer length and width in centimeters: (length × width × 0.5) grams.
| Dosage form | GEL |
| 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; use not recommended. |
| Geriatric use | No specific dose adjustment recommended; use with caution due to potential comorbidities and polypharmacy. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REGRANEX (REGRANEX).
| Breastfeeding | It is not known whether becaplermin is excreted in human milk. M/P ratio unknown. Use caution; consider developmental and health benefits of breastfeeding along with mother's clinical need for REGRANEX. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. Animal studies at doses 25-100 times human exposure show no fetal harm. Risk cannot be ruled out; use only if potential benefit justifies potential risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
Increased risk of mortality secondary to malignancy in patients treated with 3 or more tubes of REGRANEX (becaplermin) Gel. A postmarketing study showed increased mortality from cancer in patients who used three or more tubes of REGRANEX compared to control patients. REGRANEX should only be used when the benefits can be expected to outweigh the risks. REGRANEX is not recommended in patients with known malignancy.
| Serious Effects |
Known hypersensitivity to becaplermin or any product component. Application to wounds with known neoplasms or active malignancy. Use on wounds closed by primary intention.
| Precautions | Application to wounds with active malignancy may promote tumor growth. Application to wounds with infection or necrotic tissue should be discontinued until infection is controlled or necrotic tissue debrided. Potential for immunogenicity. |
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| No specific monitoring required beyond standard prenatal care. Observe for signs of wound infection or adverse effects at application site. |
| Fertility Effects | No studies on fertility in humans. In animals, no impairment of fertility observed at doses up to 25 times the human dose. |