Veldoreotide

Summary

Veldoreotide (formerly CHZ840/ZR-0080) is a next-generation, pan-somatostatin receptor analogue developed by Camurus/Novartis. It has a unique receptor binding profile covering SSTR2, SSTR4, and SSTR5, differentiating it from first-generation analogues like octreotide (SSTR2/5-selective). It is being investigated for acromegaly and neuroendocrine tumors, with a subcutaneous depot formulation using FluidCrystal technology intended to provide sustained release with less frequent dosing.

Mechanism of Action

Binds to somatostatin receptors (SSTR2, SSTR4, and SSTR5) with high affinity, inhibiting growth hormone secretion, IGF-1 production, and potentially exerting anti-proliferative effects on neuroendocrine tumor cells.

Routes of Administration

Goals & Uses

• Neuroendocrine tumor (NET) managementOncologyLow
• GH suppressionEndocrinologyModerate
• Symptom relief in carcinoid syndromeGastroenterology/OncologyLow
• IGF-1 normalizationBiomarker / Surrogate EndpointModerate
• Acromegaly controlEndocrinologyModerate

Contraindications

• Severe hepatic impairmentOrganModerateLiver function concerns
• Hypersensitivity to veldoreotide or somatostatin analoguesAllergyHigh
• PregnancyPopulationHighPotential fetal risk or insufficient safety data

Adverse Effects

• Hyperglycemia or hypoglycemiaMetabolic/EndocrineUncommon
• Injection site reactionsLocalCommon
• HeadacheNeurologicUncommonPain in the head or upper neck
• Cholelithiasis (gallstone formation)HepatobiliaryUncommon
• Gastrointestinal disturbances (nausea, diarrhea, abdominal discomfort)GastrointestinalCommon
• BradycardiaCardiovascularUncommon

Drug Interactions

• QT-prolonging drugsModerate
• CyclosporineModerate
• Bromocriptine / dopamine agonistsLow
• Insulin / Oral antidiabetic agentsModerate

Population Constraints

• Pediatric patientsAgeRelative
• Patients with hepatic impairmentOrgan FunctionRelative
• Pregnant or breastfeeding womenReproductiveRelative
• Diabetic PatientsMetabolicRelative

Regulatory Status

• European UnionInvestigationalClinical trials conducted in EU. No EMA marketing authorization granted.
• United StatesInvestigationalInvestigated under IND for acromegaly and NETs. No FDA approval as of knowledge cutoff.
• United KingdomInvestigationalNo MHRA approval; investigational status only.

Not approved in any jurisdiction as of the knowledge cutoff. Phase 2 clinical trials conducted. Investigated under IND/clinical trial frameworks in the US and EU.

Evidence & Sources

No sources recorded yet.