Veldoreotide
Also known as: CAM2029-veldoreotide, CHZ840, ZR-0080
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Summary
Veldoreotide is an investigational cyclic octapeptide somatostatin analogue that binds to somatostatin receptor subtypes 2, 4 and 5, with particularly high efficacy as an SSTR4 agonist. It is being studied for its ability to suppress hormone secretion and inhibit proliferation of neuroendocrine tumor cells. The peptide is administered subcutaneously in experimental settings and is being evaluated for conditions such as neuroendocrine tumors and disorders characterized by excess secretory activity.
Mechanism of Action
Veldoreotide binds with high affinity to somatostatin receptor subtypes 2, 4 and 5. Upon binding, it activates the G‑protein‑coupled inwardly rectifying potassium (GIRK) channels linked to these receptors, leading to membrane hyperpolarisation and downstream Gi/o signalling. This cascade reduces intracellular cyclic AMP and calcium influx, thereby suppressing secretion of chromogranin A and other neuroendocrine hormones and inhibiting cell‑cycle progression, particularly through SSTR4‑mediated pathways.
What the Research Shows
In a 2021 in‑vitro study, veldoreotide was tested in HEK293 cells engineered to express individual SSTR2, SSTR4 or SSTR5 together with GIRK2 channels, and in the neuroendocrine tumour line BON‑1 that naturally expresses these receptors. Fluorescence‑based membrane‑potential assays showed that veldoreotide produced near‑maximal activation of SSTR4 (Emax ≈ 99.5 %), far exceeding the activity of octreotide and pasireotide. It also fully activated SSTR2 and SSTR5 (Emax ≈ 98 %). In BON‑1 cells, activation of SSTR4 by veldoreotide reduced chromogranin A secretion by about 65 % and inhibited cell proliferation more effectively than native somatostatin, matching the effect of a selective SSTR4 agonist when SSTR2/5 were blocked. These data establish veldoreotide as a full agonist of SSTR2, SSTR4 and SSTR5 with pronounced SSTR4‑biased functional outcomes in neuroendocrine cell models.
Reported Benefits
Preclinical data suggest that veldoreotide can more potently activate SSTR4 than existing somatostatin analogues, leading to stronger inhibition of hormone secretion and tumour cell growth in neuroendocrine cell lines. This receptor‑biased activity may translate into therapeutic advantages for conditions where SSTR4‑mediated pathways are relevant, such as certain neuroendocrine tumours or hypersecretory disorders.
Limitations of the Evidence
Evidence is limited to cell‑based assays; no animal models, pharmacokinetic data, or clinical trials have been reported. The relevance of the observed in‑vitro potency to human disease remains uncertain, and the broader safety and efficacy profile of veldoreotide has not been established.
Safety Considerations
The published study did not report any adverse cellular effects beyond the intended antiproliferative activity. Because no in‑vivo or human data are available, the safety, tolerability and potential off‑target effects of veldoreotide remain unknown and will require systematic evaluation in future studies.
How It Is Administered
Veldoreotide is classified as an investigational peptide administered by subcutaneous injection in experimental settings. Formulation details were not described in the available literature.
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
- Journal ArticleLowDasgupta P, Gűnther T, Schulz S2021-01-01T00:00:00.000000Z
Frequently Asked Questions
What type of compound is veldoreotide?
Veldoreotide is a synthetic cyclic octapeptide that mimics somatostatin and is designed to activate somatostatin receptors, especially subtype 4.
How does veldoreotide differ from other somatostatin analogues?
In cell‑based assays, veldoreotide shows near‑full activation of SSTR4, whereas commonly used analogues such as octreotide and pasireotide have much lower activity at this receptor, suggesting a more SSTR4‑biased pharmacology.
Has veldoreotide been approved for any medical use?
No. Veldoreotide is currently an investigational compound and has not received regulatory approval for any indication.
What experimental evidence supports its potential therapeutic use?
In vitro studies demonstrated that veldoreotide reduces chromogranin A secretion and inhibits proliferation of neuroendocrine tumour cells, effects that are stronger than those of native somatostatin and comparable to a selective SSTR4 agonist.
What are the known safety concerns with veldoreotide?
The published research did not report adverse effects, but because no animal or human studies have been conducted, the safety profile of veldoreotide remains undetermined.
What is Veldoreotide?
Veldoreotide is an investigational cyclic octapeptide somatostatin analogue that binds to somatostatin receptor subtypes 2, 4 and 5, with particularly high efficacy as an SSTR4 agonist. It is being studied for its ability to suppress hormone secretion and inhibit proliferation of neuroendocrine tumor cells. The peptide is administered subcutaneously in experimental settings and is being evaluated for conditions such as neuroendocrine tumors and disorders characterized by excess secretory activity.
What is Veldoreotide used for?
Veldoreotide is educationally associated with: Neuroendocrine tumor (NET) management, GH suppression, Symptom relief in carcinoid syndrome, IGF-1 normalization, Acromegaly control. Educational only — not medical advice.
How is Veldoreotide administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Veldoreotide?
Reported adverse effects include: Hyperglycemia or hypoglycemia, Injection site reactions, Headache, Cholelithiasis (gallstone formation), Gastrointestinal disturbances (nausea, diarrhea, abdominal discomfort), Bradycardia. This list is not exhaustive — consult a qualified clinician.
Who should avoid Veldoreotide?
Recorded contraindications: Severe hepatic impairment, Hypersensitivity to veldoreotide or somatostatin analogues, Pregnancy. Consult a qualified clinician before use.