Fibroblast growth factor-1
Also known as: Acidic fibroblast growth factor, aFGF, ECGF, Endothelial cell growth factor, FGF-1, FGF‑1, FGF1, HBGF-1
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Summary
Fibroblast growth factor‑1 (FGF‑1, also called acidic FGF) is an endogenous protein that promotes cell proliferation, angiogenesis, and tissue remodeling. It is being investigated for therapeutic use in conditions such as peripheral arterial disease, type‑2 diabetes, and bone disorders, but it remains an investigational compound without regulatory approval.
Mechanism of Action
FGF‑1 binds to fibroblast growth factor receptors (primarily FGFR1) together with heparan‑sulfate proteoglycans on the cell surface. This activates downstream MAPK/ERK and PI3K/AKT pathways, stimulating endothelial cell proliferation, new‑blood‑vessel formation, and extracellular‑matrix remodeling. In adipose tissue and brain, FGF‑1 signaling enhances tissue plasticity, reduces lipolysis and improves insulin signaling. Some FGF‑1 molecules can be internalized and translocate to the nucleus, where they may directly influence gene transcription.
What the Research Shows
Pre‑clinical studies describe FGF‑1 as a local growth factor that participates in bone remodeling alongside other hormones and cytokines. Metabolic research shows that adipose‑derived and brain‑derived FGF‑1 rise after dietary stress and that peripheral or central administration of recombinant FGF‑1 lowers blood glucose, suppresses lipolysis and improves insulin sensitivity, suggesting a role in type‑2 diabetes treatment. A gene‑therapy product (riferminogene pecaplasmide, NV1FGF) delivers the FGF‑1 gene to muscle, promoting angiogenesis; it is being evaluated in a multinational, double‑blind, placebo‑controlled phase III trial for peripheral arterial disease. Additional work indicates nuclear translocation of FGF‑1 may affect transcription, but functional relevance in humans remains unclear.
Reported Benefits
Evidence from animal models suggests FGF‑1 can stimulate new blood‑vessel growth, which may improve perfusion in peripheral arterial disease. Recombinant or engineered FGF‑1 variants have shown glucose‑lowering and insulin‑sensitizing effects in pre‑clinical metabolic studies, indicating potential for type‑2 diabetes therapy. Its involvement in bone remodeling points to possible benefits for osteoporosis, although direct therapeutic data are lacking.
Limitations of the Evidence
Most data are from rodent or in‑vitro experiments; human efficacy is demonstrated only by an ongoing phase III gene‑therapy trial for PAD, whose results are not yet published. The metabolic benefits are limited to pre‑clinical observations, and the relevance of nuclear FGF‑1 actions in disease is speculative. Mitogenic activity raises concerns about uncontrolled cell proliferation, and the long‑term safety of systemic FGF‑1 exposure has not been established.
Safety Considerations
The abstracts do not report specific adverse events. Potential safety concerns stem from FGF‑1’s strong mitogenic properties, which could theoretically promote tumor growth or abnormal tissue proliferation. Gene‑therapy delivery may carry risks of insertional mutagenesis or immune reactions. Until trial results are available, the overall safety profile remains uncertain, and use should be limited to controlled research settings.
How It Is Administered
FGF‑1 has been investigated via several routes, including intracoronary infusion, intramuscular injection (as a gene‑therapy vector), intravenous infusion, and topical application. Formulations range from recombinant protein preparations to plasmid‑based gene‑therapy constructs that drive local expression of the growth factor.
Routes of Administration
Goals & Uses
- Neural tissue repair and neuroprotectionNeurologyLow
- Angiogenesis promotion in coronary artery diseaseCardiovascularModerate
- Diabetic wound healingDermatology/MetabolicModerate
- Peripheral arterial disease / critical limb ischemiaVascularModerate
- Wound healingDermatologicModerateTissue repair and wound healing
- Metabolic syndrome / insulin sensitizationMetabolicLow
- Cardiac ischemia protectionCardiologyModerate
- Peripheral nerve regenerationNeurologicalLow
Contraindications
- Active malignancyOncologyHighUse caution or avoid depending on agent and context
- PregnancyPopulationModeratePotential fetal risk or insufficient safety data
- Proliferative RetinopathyOphthalmologyModerate
- History of solid organ malignancyOncologyHigh
Adverse Effects
- ProteinuriaRenalUncommon
- Injection site reactionsLocalCommon
- HypotensionCardiovascularUnknownLow blood pressure
- Fever / flu-like symptomsSystemicUncommon
- Theoretical Oncogenic RiskOncologyUnknown
Drug Interactions
- HeparinLow
- Anticoagulants (warfarin, DOACs)Moderate
- Bevacizumab (anti-VEGF agents)Moderate
Population Constraints
- Patients with diabetes mellitus (with retinopathy)ComorbidityRelative
- Pediatric patientsAgeRelative
- Immunocompromised patientsImmunologicRelative
- Pregnant womenReproductiveRelative
- Patients with FGFR-mutant cancersOncology/GeneticAbsolute
Regulatory Status
- European UnionInvestigationalUnder clinical investigation for diabetic foot ulcer treatment.
- United StatesInvestigationalInvestigational use in clinical trials for wound healing.
- United KingdomUnknownNo MHRA-approved FGF-1 product identified; treated as investigational.
No FDA, EMA, or MHRA-approved therapeutic product based solely on FGF-1 as of 2024. Various recombinant forms and gene therapy vectors encoding FGF-1 have entered clinical trials (e.g., NV1FGF/Generx for coronary artery disease). Trafermin (recombinant FGF-2) is sometimes confused with FGF-1; they are distinct. Classified as a research/investigational agent.
Evidence & Sources
- Journal ArticleModerateBonucci E, Ballanti P2014-01-01T00:00:00.000000Z
- Journal ArticleModerateGasser E, et al.2022-01-01T00:00:00.000000Z
- Journal ArticleModerate2010-01-01T00:00:00.000000Z
- Journal ArticleModerateSilver J, Naveh-Many T2012-01-01T00:00:00.000000Z
- Journal ArticleModerateProchiantz A, Théodore L1995-01-01T00:00:00.000000Z
Frequently Asked Questions
What conditions is FGF‑1 being studied for?
FGF‑1 is under investigation for peripheral arterial disease (using a gene‑therapy approach), metabolic disorders such as type‑2 diabetes (via recombinant protein or engineered variants), and bone‑remodeling disorders like osteoporosis, based mainly on pre‑clinical data.
Has FGF‑1 been approved for any medical use?
No. All current applications of FGF‑1 are investigational; it has not received regulatory approval for any indication.
How is FGF‑1 delivered in clinical trials?
In the PAD trial, a plasmid encoding FGF‑1 (riferminogene pecaplasmide) is injected intramuscularly, where muscle cells produce the protein locally. Other experimental routes include intravenous, intracoronary, and topical delivery of recombinant protein.
What are the main safety concerns with FGF‑1 therapy?
Because FGF‑1 promotes cell proliferation, there is theoretical risk of abnormal tissue growth or tumorigenesis. Gene‑therapy vectors may also provoke immune responses or insertional mutagenesis. No definitive adverse‑event data are available from the cited literature.
Is there evidence that FGF‑1 improves bone health?
FGF‑1 is listed among local growth factors that regulate bone remodeling in animal models, but no direct therapeutic studies in humans have been reported in the provided abstracts.
What is Fibroblast growth factor-1?
Fibroblast growth factor‑1 (FGF‑1, also called acidic FGF) is an endogenous protein that promotes cell proliferation, angiogenesis, and tissue remodeling. It is being investigated for therapeutic use in conditions such as peripheral arterial disease, type‑2 diabetes, and bone disorders, but it remains an investigational compound without regulatory approval.
What is Fibroblast growth factor-1 used for?
Fibroblast growth factor-1 is educationally associated with: Neural tissue repair and neuroprotection, Angiogenesis promotion in coronary artery disease, Diabetic wound healing, Peripheral arterial disease / critical limb ischemia, Wound healing, Metabolic syndrome / insulin sensitization, Cardiac ischemia protection, Peripheral nerve regeneration. Educational only — not medical advice.
How is Fibroblast growth factor-1 administered?
Recorded routes of administration: Intracoronary, Intramuscular, Intravenous, Subcutaneous, Topical.
What are the potential side effects of Fibroblast growth factor-1?
Reported adverse effects include: Proteinuria, Injection site reactions, Hypotension, Fever / flu-like symptoms, Theoretical Oncogenic Risk. This list is not exhaustive — consult a qualified clinician.
Who should avoid Fibroblast growth factor-1?
Recorded contraindications: Active malignancy, Pregnancy, Proliferative Retinopathy, History of solid organ malignancy. Consult a qualified clinician before use.