Eflapegrastim

Summary

Eflapegrastim (Rolvedon) is a long-acting PEGylated G-CSF conjugate approved by the FDA in 2022 for the prevention of severe neutropenia in adult patients with non-myeloid malignancies receiving myelosuppressive chemotherapy. It is administered as a single subcutaneous injection once per chemotherapy cycle, at least 24 hours after cytotoxic chemotherapy.

Mechanism of Action

Eflapegrastim is a long-acting G-CSF receptor agonist. It consists of a G-CSF analog conjugated to an IgG4 Fc fragment via a PEG linker, which prolongs half-life. It stimulates proliferation, differentiation, and activation of neutrophil precursors, increasing neutrophil production and reducing duration of severe neutropenia.

Routes of Administration

Goals & Uses

• Reduction of febrile neutropenia riskOncology Supportive CareHigh
• Prevention of chemotherapy-induced severe neutropeniaOncology Supportive CareHigh
• Shortened duration of severe neutropeniaHematologyHigh

Contraindications

• Hypersensitivity to eflapegrastim or any componentAllergy/ImmunologyHigh
• Administration between 14 days before and 24 hours after cytotoxic chemotherapyTiming RestrictionHigh

Adverse Effects

• Acute respiratory distress syndrome (ARDS)PulmonaryRare
• Splenomegaly / splenic ruptureOrgan ToxicityRare
• Injection site reactionsLocalCommon
• LeukocytosisHematologicCommon
• AortitisCardiovascularRare
• Bone pain / musculoskeletal painMusculoskeletalCommon

Drug Interactions

• Cytotoxic chemotherapy agentsHigh
• LithiumModerate

Population Constraints

• PregnancyReproductive SafetyRelative
• Pediatric patientsAgeRelative
• LactationReproductiveRelative
• Sickle cell diseaseHematologicRelative
• Myeloid malignanciesOncologicAbsolute

Regulatory Status

• European UnionUnknownNot approved by EMA as of knowledge cutoff
• United StatesApprovedApproved: Prevention of severe neutropenia in adult patients with non-myeloid malignancies receiving myelosuppressive anticancer drugs associated with clinically significant incidence of febrile neutropeniaFDA approved September 9, 2022; BLA 761195; brand name Rolvedon
• United KingdomUnknownNot approved by MHRA as of knowledge cutoff

FDA approved September 9, 2022 under brand name Rolvedon. Developed by Spectrum Pharmaceuticals. Not yet approved in EU or UK as of knowledge cutoff.

Evidence & Sources

No sources recorded yet.