Eflapegrastim
Also known as: Eflapegrastim, eflapegrastim-xnst, HM10460A, RGL‑001, Rolvedon, SPI-2012
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Summary
Eflapegrastim is an investigational, long‑acting granulocyte colony‑stimulating factor (G‑CSF) analog designed to prevent chemotherapy‑induced neutropenia, particularly in early‑stage breast cancer patients receiving docetaxel/cyclophosphamide. It is administered by subcutaneous injection and aims to shorten the duration of severe neutropenia and reduce febrile neutropenia risk, offering a potential alternative to existing agents such as pegfilgrastim.
Mechanism of Action
Eflapegrastim consists of a recombinant human G‑CSF molecule linked to an IgG4 Fc fragment via a short polyethylene‑glycol linker. The G‑CSF domain binds the G‑CSF receptor on myeloid progenitor cells, stimulating proliferation, differentiation, and survival of neutrophil precursors. The Fc fusion extends circulating half‑life, providing sustained receptor activation and a prolonged rise in absolute neutrophil count after a single subcutaneous dose.
What the Research Shows
Clinical data are limited to breast‑cancer cohorts. A phase‑1 open‑label trial (n=53) gave eflapegrastim 0.5 h after chemotherapy and reported a mean ANC recovery time of 1.8 days, a 2 % febrile neutropenia rate, and a safety profile similar to next‑day dosing. Two pivotal phase‑3 studies (RECOVER and ADVANCE) compared a fixed 13.2 mg dose (3.6 mg G‑CSF equivalent) to pegfilgrastim 6 mg. Both demonstrated non‑inferior mean duration of severe neutropenia across cycles, with comparable adverse‑event rates. A network meta‑analysis of 33 randomized trials identified eflapegrastim 13.2 mg as among the most effective long‑acting G‑CSFs, showing high efficacy against severe neutropenia and febrile neutropenia without increased serious adverse events.
Reported Benefits
Evidence from randomized trials suggests eflapegrastim reduces the duration and incidence of severe neutropenia at a lower G‑CSF dose than pegfilgrastim, while maintaining a similar safety profile. Same‑day administration appears feasible, potentially improving convenience for patients and clinicians. The Fc‑mediated half‑life extension may allow sustained neutrophil support with a single injection per chemotherapy cycle.
Limitations of the Evidence
Data are confined to early‑stage breast cancer patients receiving docetaxel/cyclophosphamide; efficacy in other cancers or chemotherapy regimens is untested. Long‑term safety and real‑world outcomes remain unknown, as studies are limited to phase‑1 and phase‑3 trials with relatively short follow‑up. The drug remains investigational and has not received regulatory approval for any indication.
Safety Considerations
Common treatment‑emergent adverse events included bone pain, fatigue, nausea, and alopecia, mirroring other G‑CSFs. Serious adverse events were rare, and discontinuations due to drug‑related toxicity occurred in about 2 % of participants. No new safety signals emerged with same‑day dosing, but clinicians should monitor for typical G‑CSF‑related bone pain and hematologic effects.
How It Is Administered
Eflapegrastim is given by subcutaneous injection, typically as a fixed 13.2 mg dose (0.6 mL) administered either within 30 minutes after chemotherapy (same‑day protocol) or the standard 24‑hour post‑chemotherapy interval. The formulation is a sterile solution designed for single‑use administration.
Routes of Administration
Goals & Uses
- Shortening duration of severe neutropenia (DSN)OncologyModerate
- Reduction of febrile neutropenia riskOncology Supportive CareHigh
- Prevention of chemotherapy-induced severe neutropeniaOncology Supportive CareHigh
- Shortened duration of severe neutropeniaHematologyHigh
- Reduction of chemotherapy‑induced neutropeniaOncologyModerate
Contraindications
- Hypersensitivity to eflapegrastim or any excipientAllergyHigh
- Patients with known myeloid malignancies (e.g., CML, AML) in blast phaseOncologyModerate
- 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
- Bone painMusculoskeletalCommon
- Injection site reactionsLocalCommon
- LeukocytosisHematologicCommon
- Splenic ruptureGastrointestinal/HematologicRare
- Injection‑site reactionsLocalCommon
- AortitisCardiovascularRare
- Bone pain / musculoskeletal painMusculoskeletalCommon
Drug Interactions
- Cytotoxic chemotherapy agentsHigh
- LithiumModerate
- Concurrent myelosuppressive chemotherapyModerate
Population Constraints
- PregnancyReproductive SafetyRelative
- Pediatric patientsAgeRelative
- LactationReproductiveRelative
- Pregnant or breastfeeding womenReproductiveRelative
- Sickle cell diseaseHematologicRelative
- Myeloid malignanciesOncologicAbsolute
- Pediatric patients <2 yearsAgeRelative
Regulatory Status
- European UnionUnknownNo marketing authorization granted yet.
- United StatesInvestigationalPhase III data submitted; FDA decision pending as of 2024.
- 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
- Journal ArticleModerateModiano M, et al.2025-01-01T00:00:00.000000Z
- Journal ArticleModerateBlayney DW, Schwartzberg L2022-01-01T00:00:00.000000Z
- Journal ArticleModerateCobb PW, et al.2020-01-01T00:00:00.000000Z
- Journal ArticleModerateYou Z, et al.2023-01-01T00:00:00.000000Z
- Journal ArticleLowMoon YW, et al.2023-01-01T00:00:00.000000Z
Frequently Asked Questions
What type of chemotherapy regimens has eflapegrastim been studied with?
Clinical trials have evaluated eflapegrastim in patients receiving docetaxel plus cyclophosphamide (TC) as neoadjuvant or adjuvant therapy for early‑stage breast cancer. No published data assess its use with other chemotherapy combinations.
How does eflapegrastim compare to pegfilgrastim in effectiveness?
Phase‑3 trials showed eflapegrastim was non‑inferior to pegfilgrastim in reducing the mean duration of severe neutropenia across treatment cycles, with similar rates of febrile neutropenia and comparable safety outcomes, despite delivering a lower G‑CSF dose.
Can eflapegrastim be given on the same day as chemotherapy?
A phase‑1 study administering eflapegrastim 0.5 hours after docetaxel/cyclophosphamide reported rapid neutrophil recovery and low febrile neutropenia incidence, suggesting same‑day dosing is feasible and well tolerated.
What are the most common side effects?
The most frequently reported adverse events are bone pain, fatigue, nausea, and alopecia, which are typical of G‑CSF therapy. Serious adverse events were rare, and drug‑related discontinuations occurred in about 2 % of participants.
Is eflapegrastim approved for clinical use?
No. Eflapegrastim is currently classified as an investigational compound and has not received regulatory approval for any therapeutic indication.
What is Eflapegrastim?
Eflapegrastim is an investigational, long‑acting granulocyte colony‑stimulating factor (G‑CSF) analog designed to prevent chemotherapy‑induced neutropenia, particularly in early‑stage breast cancer patients receiving docetaxel/cyclophosphamide. It is administered by subcutaneous injection and aims to shorten the duration of severe neutropenia and reduce febrile neutropenia risk, offering a potential alternative to existing agents such as pegfilgrastim.
What is Eflapegrastim used for?
Eflapegrastim is educationally associated with: Shortening duration of severe neutropenia (DSN), Reduction of febrile neutropenia risk, Prevention of chemotherapy-induced severe neutropenia, Shortened duration of severe neutropenia, Reduction of chemotherapy‑induced neutropenia. Educational only — not medical advice.
How is Eflapegrastim administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Eflapegrastim?
Reported adverse effects include: Acute respiratory distress syndrome (ARDS), Splenomegaly / splenic rupture, Bone pain, Injection site reactions, Leukocytosis, Splenic rupture, Injection‑site reactions, Aortitis, Bone pain / musculoskeletal pain. This list is not exhaustive — consult a qualified clinician.
Who should avoid Eflapegrastim?
Recorded contraindications: Hypersensitivity to eflapegrastim or any excipient, Patients with known myeloid malignancies (e.g., CML, AML) in blast phase, Hypersensitivity to eflapegrastim or any component, Administration between 14 days before and 24 hours after cytotoxic chemotherapy. Consult a qualified clinician before use.