Talabostat
Also known as: L-valyl-L-boroproline, PT-100, PT‑100, Talabostat, Val-boroPro, Val‑boroPro
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Summary
Talabostat (Val‑boroPro, PT‑100) is a small‑molecule dipeptide boronic acid that blocks DPP‑IV and related enzymes. It has been studied in oncology and inflammatory diseases but has never received regulatory approval.
Mechanism of Action
Reversible covalent inhibition of dipeptidyl peptidases DPP‑IV, DPP‑8/9 and fibroblast activation protein, modulating immune and inflammatory pathways
Routes of Administration
Goals & Uses
- Solid tumor oncologyOncologyModerate
- Colorectal cancer treatmentOncologyModerate
- Combination immunotherapy enhancementOncologyLow
- ImmunomodulationImmunologyModerate
- Metastatic melanoma treatmentOncologyModerate
- NLRP1 inflammasome activation researchImmunology/researchHigh
- Anti-tumor immunostimulationOncologyModerate
- Inflammatory bowel diseaseGastroenterologyLow
- Hematologic malignancy treatmentOncologyLow
Contraindications
- Uncontrolled infectionInfectious DiseaseModerate
- Severe hepatic impairmentOrganHighLiver function concerns
- Known hypersensitivity to boronic‑acid compoundsAllergyModerate
- Severe inflammatory syndromeImmunologicHigh
- Active autoimmune diseaseAutoimmunityHigh
Adverse Effects
- Cytokine release / flu-like symptomsImmunologicCommon
- ThrombocytopeniaHematologicUncommonLow platelet count
- Edema (peripheral/facial)Fluid/electrolyteCommon
- AnemiaHematologicUncommonLow red blood cell count or hemoglobin
- HypotensionCardiovascularCommonLow blood pressure
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- FatigueGeneralCommonLow energy or tiredness
- VomitingGastrointestinalCommonForceful expulsion of stomach contents
- Elevated liver enzymesHepaticUncommonIncrease in AST/ALT or other hepatic markers
Drug Interactions
- Other DPP‑IV inhibitorsHigh
- Immunosuppressants (e.g., corticosteroids)Moderate
- Antihypertensive agentsModerate
- Other DPP4 inhibitors (gliptins)Moderate
- Insulin or sulfonylureasModerate
Population Constraints
- Pediatric patientsAgeRelative
- Elderly patients (≥75 years)AgeRelative
- Pregnant or lactating womenReproductiveAbsolute
- Patients with severe hepatic impairmentHepaticRelative
- Pregnant womenReproductiveAbsolute
Regulatory Status
- European UnionInvestigationalNo marketing authorization.
- United StatesInvestigationalNever submitted for NDA; discontinued development.
- United KingdomInvestigationalNo approval; only used in research.
Investigational agent; clinical development discontinued after phase II due to limited efficacy and safety concerns.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Talabostat?
Talabostat (Val‑boroPro, PT‑100) is a small‑molecule dipeptide boronic acid that blocks DPP‑IV and related enzymes. It has been studied in oncology and inflammatory diseases but has never received regulatory approval.
What is Talabostat used for?
Talabostat is educationally associated with: Solid tumor oncology, Colorectal cancer treatment, Combination immunotherapy enhancement, Immunomodulation, Metastatic melanoma treatment, NLRP1 inflammasome activation research, Anti-tumor immunostimulation, Inflammatory bowel disease, Hematologic malignancy treatment. Educational only — not medical advice.
How is Talabostat administered?
Recorded routes of administration: Intravenous, Oral.
What are the potential side effects of Talabostat?
Reported adverse effects include: Cytokine release / flu-like symptoms, Thrombocytopenia, Edema (peripheral/facial), Anemia, Hypotension, Nausea, Fatigue, Vomiting, Elevated liver enzymes. This list is not exhaustive — consult a qualified clinician.
Who should avoid Talabostat?
Recorded contraindications: Uncontrolled infection, Severe hepatic impairment, Known hypersensitivity to boronic‑acid compounds, Severe inflammatory syndrome, Active autoimmune disease. Consult a qualified clinician before use.