Palifermin Advanced Drug Monograph

Palifermin Report

Name: Palifermin Name (English): Palifermin DrugBank ID: DB00039 Type: Biotech CAS Number: 162394-19-6

Palifermin is a recombinant human keratinocyte growth factor (KGF) comprised of 140 amino acid residues. It is produced using E. coli. Palifermin binds to the human keratinocyte growth factor (KGF) receptor on epithelial cell surfaces. This action stimulates epithelial cell proliferation, differentiation, and migration, thereby protecting and promoting healing of tissues lining the mouth and gastrointestinal tract.

Indication: To decrease the incidence, duration, and severity of oral mucositis in adult patients with hematologic malignancies receiving myeloablative radiochemotherapy requiring hematopoietic stem cell support.

Pharmacology: Palifermin acts as both a cell growth and survival factor. It promotes cell proliferation and upregulates cytoprotective mechanisms.

Contraindications: No specific contraindications are listed in the provided data.

Adverse Effects: Common side effects include thickening of oral mucosa, flushing, and dysgeusia. Other reported side effects include swelling, pain (including joint pain), increase in blood pancreas enzymes, increased blood pressure, and proteinuria. Serious side effects may include difficulty breathing and changes in cutaneous or mucous membrane appearance/feel.

Drug Interactions: Therapeutic efficacy of Palifermin may be decreased when used in combination with arsenic trioxide, azacitidine, belinostat, bendamustine, cabazitaxel, capecitabine, carfilzomib, carmustine, cytarabine, dacarbazine, dactinomycin, daunorubicin, decitabine, docetaxel, doxorubicin, epirubicin, eribulin, etoposide, floxuridine, fludarabine, fluorouracil, gemcitabine, idarubicin, ifosfamide, irinotecan, ixabepilone, lomustine, mechlorethamine, melphalan, mercaptopurine, methotrexate, mitomycin, mitoxantrone, nelarabine, oxaliplatin, paclitaxel, pemetrexed, pentostatin, procarbazine, raltitrexed, teniposide, thioguanine, topotecan, trabectedin, tretinoin, uracil mustard, valrubicin, vinblastine, vincristine, vindesine, vinorelbine. Serum concentration of Palifermin may be increased when combined with bemiparin, dalteparin, enoxaparin, heparin, and tinzaparin.

Mechanism of Action: Palifermin binds to KGF receptors, stimulating epithelial cell proliferation, differentiation, and migration, which contributes to the protection and regeneration of mucosal tissues damaged by chemotherapy and radiation.

Absorption: Not Available.

Half-life: Elimination half-life is approximately 4.5 hours (range: 3.3-5.7 hours).

Metabolism: Not Available.

Route of Administration: Intravenous bolus injection.

Dosage: The recommended dose is 60 µg/kg/day administered as an intravenous bolus injection for three consecutive days before and three consecutive days after myelotoxic therapy. Palifermin should not be administered within 24 hours before, during, or after administration of chemotherapy.

Formulation: Lyophilized powder for reconstitution with sterile water for injection.

Storage: Specific storage instructions should be followed as per the product labeling.

Precautions: Palifermin has been shown to enhance the growth of human epithelial tumor cell lines in vitro and in animal studies. Although clinical studies have not shown an increased incidence of malignancy, caution should be exercised in patients with pre-existing malignancies.

Therapeutic Category: Mucocutaneous Epithelial Cell Growth Factor.

Additional Information: Palifermin is a recombinant form of the endogenous human keratinocyte growth factor. It is approved by the FDA and EMA.