Dopastatin
Also known as: BIM-23268, BIM-23A387, BIM-23A760, chimeric SST-DA agonist
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Summary
Dopastatin is a research‑stage chimeric peptide that combines a somatostatin analogue with a dopamine‑D2 receptor agonist. It is being investigated for disorders in which excess pituitary hormone secretion or neuroendocrine tumour growth is driven by somatostatin and dopamine receptor pathways, such as acromegaly, prolactin‑secreting adenomas, Cushing’s disease and gastro‑entero‑pancreatic neuroendocrine tumours. The compound remains experimental, with no regulatory approval for any indication.
Mechanism of Action
Dopastatin binds to somatostatin receptor subtype 2 (SSTR2) and dopamine D2 receptors on pituitary and neuroendocrine cells. Activation of SSTR2 couples to Gi proteins, inhibiting adenylyl cyclase, reducing cAMP, and suppressing calcium‑dependent hormone release. D2‑receptor activation produces a similar Gi‑mediated signal, further lowering cAMP and calcium influx. The combined signalling leads to decreased secretion of growth hormone, prolactin, ACTH and other peptide hormones, and triggers antiproliferative pathways that cause cell‑cycle arrest and apoptosis in tumour cells.
What the Research Shows
The literature mentions dopastatin as a promising chimeric agent in several reviews of pituitary adenoma and neuroendocrine tumour therapy. Early in‑vitro studies reported dose‑dependent inhibition of cell replication in about 60 % of pituitary adenoma cultures, and greater potency than cabergoline in prolactin‑secreting tumours. Reviews of emerging treatments for Cushing’s disease and gastro‑entero‑pancreatic NETs cite dopastatin as a candidate to be introduced into clinical practice, but no patient trials are described. A phase‑1 study of a related somatostatin‑dopamine chimera (BIM23B065) in healthy men demonstrated clear reductions in endogenous growth‑hormone and prolactin secretion, providing proof of concept for the dual‑receptor approach, yet direct clinical data on dopastatin itself are lacking.
Reported Benefits
Preclinical data suggest dopastatin can suppress excessive pituitary hormone output and inhibit tumour cell proliferation more efficiently than single‑receptor agents. In vitro experiments showed hormone‑secretion blockade and growth inhibition at concentrations far lower than those required for separate somatostatin or dopamine agonists. The dual‑target design may overcome resistance linked to variable receptor expression, offering a theoretical advantage for patients whose adenomas express both SSTR2 and D2 receptors.
Limitations of the Evidence
Evidence for dopastatin is limited to laboratory studies and expert commentary; no controlled clinical trials in patients have been reported. Its efficacy depends on co‑expression of SSTR2 and D2 receptors, which varies among tumour types. The related phase‑1 chimera studied in healthy volunteers does not establish therapeutic benefit or safety in disease states. Consequently, the true clinical value, optimal dosing, and long‑term outcomes remain undefined.
Safety Considerations
No adverse‑event data specific to dopastatin are available in the cited literature. The phase‑1 study of a similar chimera reported only pharmacodynamic effects without mentioning safety concerns, but the small healthy‑volunteer population limits conclusions. Potential side‑effects may resemble those of somatostatin analogues (e.g., gastrointestinal discomfort, gallstone formation) and dopamine agonists (e.g., nausea, orthostatic hypotension), yet these remain speculative until formal safety assessments are performed.
How It Is Administered
Dopastatin is described as being administered by intravenous or subcutaneous injection. Formulation details are not provided in the available sources, and dosing regimens have not been established in clinical studies.
Routes of Administration
Goals & Uses
- Overcoming somatostatin analog resistancePharmacologicalModerate
- Prolactin suppressionEndocrineModerate
- Treatment of neuroendocrine tumorsOncologyLow
- Reduction of growth hormone hypersecretion in acromegalyEndocrineModerate
Contraindications
- Severe hepatic impairmentOrganModerateLiver function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Hypersensitivity to somatostatin analogs or dopamine agonistsAllergy/ImmunologyHigh
Adverse Effects
- Injection site reactionsLocalCommon
- CholelithiasisHepatobiliaryUncommon
- Gastrointestinal disturbances (nausea, diarrhea, abdominal cramping)GastrointestinalCommon
- Orthostatic hypotensionCardiovascularUncommon
- Nausea and vomitingGastrointestinalCommon
- Hypoglycemia or hyperglycemiaMetabolicUncommon
Drug Interactions
- CyclosporineModerate
- Antidiabetic agents (insulin, sulfonylureas)Moderate
- Dopamine antagonists (e.g., haloperidol, metoclopramide)Moderate
Population Constraints
- Pediatric patientsAgeRelative
- Patients with Parkinson's disease on dopaminergic therapyNeurologicalRelative
- Elderly patients (>75 years)AgeRelative
Regulatory Status
- European UnionInvestigationalNo EMA approval; clinical investigations conducted in European centers.
- United StatesInvestigationalNo FDA approval; studied under IND/clinical trial frameworks for acromegaly.
- United KingdomInvestigationalNo MHRA approval; research/trial use only.
No regulatory approval in any jurisdiction as of current knowledge cutoff. Investigational use only; studied in Phase I/II clinical trials for acromegaly and neuroendocrine tumors.
Evidence & Sources
- Journal ArticleModerateCuevas-Ramos D, Fleseriu M2014-01-01T00:00:00.000000Z
- Journal ArticleModerateOberg K2009-01-01T00:00:00.000000Z
- Journal ArticleModerateTheodoropoulou M, Stalla GK2013-01-01T00:00:00.000000Z
- Journal ArticleModeratevan Aken MO, et al.2006-01-01T00:00:00.000000Z
- Journal ArticleModerateDrutel A, Caron P, Archambeaud F2008-01-01T00:00:00.000000Z
- Journal ArticleModeratevan Esdonk MJ, et al.2020-01-01T00:00:00.000000Z
Frequently Asked Questions
What conditions is dopastatin being studied for?
The compound is being explored for hormone‑secreting pituitary adenomas (such as acromegaly and prolactinomas), Cushing’s disease caused by ACTH‑producing tumours, and gastro‑entero‑pancreatic neuroendocrine tumours that express somatostatin and dopamine receptors.
Has dopastatin been tested in patients?
No patient trials are reported in the cited literature. Existing information comes from in‑vitro experiments, expert reviews, and a phase‑1 study of a related chimera in healthy volunteers, which only demonstrates pharmacological activity, not therapeutic efficacy.
How does dopastatin differ from existing drugs like octreotide or cabergoline?
Octreotide targets somatostatin receptors, mainly SSTR2, while cabergoline activates dopamine D2 receptors. Dopastatin combines both activities in a single molecule, aiming to achieve stronger hormone suppression and antiproliferative effects, especially when tumours express both receptor types.
Is dopastatin approved for any medical use?
No. The structured data and abstracts indicate that dopastatin remains in the research phase and has not received regulatory approval for any indication.
What are the known side effects of dopastatin?
Specific side‑effect information for dopastatin is not available. Potential adverse effects are inferred from its component activities and may include gastrointestinal symptoms, gallstone risk, nausea, and blood‑pressure changes, but these remain unconfirmed.
What is Dopastatin?
Dopastatin is a research‑stage chimeric peptide that combines a somatostatin analogue with a dopamine‑D2 receptor agonist. It is being investigated for disorders in which excess pituitary hormone secretion or neuroendocrine tumour growth is driven by somatostatin and dopamine receptor pathways, such as acromegaly, prolactin‑secreting adenomas, Cushing’s disease and gastro‑entero‑pancreatic neuroendocrine tumours. The compound remains experimental, with no regulatory approval for any indication.
What is Dopastatin used for?
Dopastatin is educationally associated with: Overcoming somatostatin analog resistance, Prolactin suppression, Treatment of neuroendocrine tumors, Reduction of growth hormone hypersecretion in acromegaly. Educational only — not medical advice.
How is Dopastatin administered?
Recorded routes of administration: Intravenous, Subcutaneous.
What are the potential side effects of Dopastatin?
Reported adverse effects include: Injection site reactions, Cholelithiasis, Gastrointestinal disturbances (nausea, diarrhea, abdominal cramping), Orthostatic hypotension, Nausea and vomiting, Hypoglycemia or hyperglycemia. This list is not exhaustive — consult a qualified clinician.
Who should avoid Dopastatin?
Recorded contraindications: Severe hepatic impairment, Pregnancy, Hypersensitivity to somatostatin analogs or dopamine agonists. Consult a qualified clinician before use.