REGRANEX
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 25235 |
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 | Becaplermin is a platelet-derived growth factor. No adequate and well-controlled studies in pregnant women. Animal reproduction studies have not been conducted. Risk cannot be ruled out. |
| 2nd trimester | No human data available. Use only if clearly needed and potential benefit justifies potential risk to fetus. |
| 3rd trimester | No human data available. Use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for REGRANEX (REGRANEX).
| Placental transfer | Molecular weight (~25 kDa) suggests limited placental transfer, but no human data available. Large protein likely does not cross placenta in significant amounts. |
| Breastfeeding | It is not known whether becaplermin is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. |
| Lactation Rating | L3 (Moderately Safe) |
| 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 | 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. |
■ 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 component of the productNeoplasms at the site of application
| 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. |
| Food/Dietary | No known food interactions. Regranex is applied topically and has minimal systemic absorption. |
| Clinical Pearls | Regranex (becaplermin) is a recombinant platelet-derived growth factor (PDGF) gel indicated for diabetic neuropathic ulcers extending into subcutaneous tissue or deeper. Ensure ulcer is free of infection, necrotic tissue, and has adequate blood supply before initiating therapy. Apply a thin layer once daily, and recalibrate gel amount based on ulcer dimensions (length x width x 0.5 for cm to grams). Do not use on wounds with exposed bone, tendon, or joint. Monitor for increased risk of malignancy; contraindicated in patients with active malignancies. The gel is for single-patient use only; discard tube 30 days after opening. |
| Patient Advice | Wash hands before and after applying Regranex. · Clean the ulcer gently with saline or water before each application. · Apply a thin layer of gel (about 1/16 inch) to the entire ulcer area once daily. · Cover the ulcer with a saline-moistened gauze dressing after applying gel. · Do not use more than the prescribed amount or frequency. · Store Regranex in the refrigerator; do not freeze. · Discard any unused gel in the tube 30 days after first opening. · Report any signs of infection (increased pain, redness, swelling, foul odor) or new skin changes around the wound. · You may need to have your wound measured weekly to adjust the gel amount. · Avoid applying other creams, ointments, or lotions to the same area. |
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