SF1126
Also known as: cRGD‑PEG‑LY294002, LY294002-RGDS conjugate, SF 1126, SF1126
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Summary
SF1126 is a PEGylated cyclic RGD peptide conjugated to the PI3K inhibitor LY294002, designed for integrin‑mediated delivery of a PI3K/mTOR inhibitor to cancer cells; evaluated in early‑phase oncology trials.
Mechanism of Action
cRGD motif targets αvβ3/αvβ5 integrins, delivering the LY294002 moiety to tumor cells and inhibiting PI3K/AKT/mTOR signaling
Routes of Administration
Goals & Uses
- Treatment of B-cell malignancies (CLL, B-cell NHL)Oncology / HematologyLow
- Tumor growth inhibitionOncologyModerate
- Treatment of advanced solid tumorsOncologyLow
- PI3K/Akt/mTOR pathway blockadeSignal Transduction InhibitionModerate
- Tumor angiogenesis inhibitionOncology / AntiangiogenicModerate
Contraindications
- Severe hepatic impairmentOrganModerateLiver function concerns
- Known hypersensitivity to peptide or PEG componentsAllergyModerate
- Known hypersensitivity to LY294002 or RGDS componentsAllergyHigh
- Active uncontrolled infectionInfectious DiseaseModerate
Adverse Effects
- HyperglycemiaMetabolicCommonAbnormally high blood glucose
- ThrombocytopeniaHematologicUncommonLow platelet count
- Nausea/vomitingGastrointestinalCommon
- Infusion‑related reactionsGeneralCommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- FatigueGeneralCommonLow energy or tiredness
- Elevated liver enzymes (transaminases)HepaticUncommon
- Infusion-related reactionsHypersensitivityUncommon
- DiarrheaGastrointestinalUncommonLoose or frequent stools
Drug Interactions
- CYP3A4 inhibitorsModerate
- Antidiabetic agents (insulin, metformin)Moderate
- Anticoagulants (warfarin, heparin)Moderate
- CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)Moderate
Population Constraints
- PregnancyReproductive SafetyAbsolute
- Pediatric patientsAgeRelative
- Patients with diabetes mellitusMetabolicRelative
- PediatricsAgeRelative
Regulatory Status
- European UnionUnknownNo marketing authorization; clinical studies ongoing.
- United StatesInvestigationalIND; Phase I/II trials in solid tumors.
- United KingdomUnknownNo MHRA approval documented.
IND status in the United States; no approved indication in any jurisdiction.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is SF1126?
SF1126 is a PEGylated cyclic RGD peptide conjugated to the PI3K inhibitor LY294002, designed for integrin‑mediated delivery of a PI3K/mTOR inhibitor to cancer cells; evaluated in early‑phase oncology trials.
What is SF1126 used for?
SF1126 is educationally associated with: Treatment of B-cell malignancies (CLL, B-cell NHL), Tumor growth inhibition, Treatment of advanced solid tumors, PI3K/Akt/mTOR pathway blockade, Tumor angiogenesis inhibition. Educational only — not medical advice.
How is SF1126 administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of SF1126?
Reported adverse effects include: Hyperglycemia, Thrombocytopenia, Nausea/vomiting, Infusion‑related reactions, Nausea, Fatigue, Elevated liver enzymes (transaminases), Infusion-related reactions, Diarrhea. This list is not exhaustive — consult a qualified clinician.
Who should avoid SF1126?
Recorded contraindications: Severe hepatic impairment, Known hypersensitivity to peptide or PEG components, Known hypersensitivity to LY294002 or RGDS components, Active uncontrolled infection. Consult a qualified clinician before use.