Insulinoma Medication

Updated: May 31, 2020
  • Author: Zonera Ashraf Ali, MBBS; Chief Editor: Neetu Radhakrishnan, MD  more...
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Medication

Medication Summary

Diazoxide is the drug of choice because it inhibits insulin release from the tumor. Adverse effects must be treated with hydrochlorothiazide. In patients not responsive to or intolerant of diazoxide (10%), a somatostatin analog may be indicated to prevent hypoglycemia.

Experience with systemic chemotherapy is limited. The traditional regimen of choice has been streptozocin and doxorubicin. Response rates as high as 69% have been reported but radiologic response is lower and due to uncertainty about efficacy and increased toxicity, this regimen is not accepted as a standard first-line therapy.

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Hyperglycemic agents

Class Summary

Inhibit insulin release from the tumor.

Diazoxide (Proglycem, Hyperstat)

Produces an increase in blood glucose within 1 h by inhibition of insulin release from the insulinoma.

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Diuretics

Class Summary

Used to counteract edema and hyperkalemia secondary to diazoxide and to potentiate its hyperglycemic effect.

Hydrochlorothiazide (Microzide, HydroDIURIL, Esidrix)

Inhibits reabsorption of sodium in distal tubules, causing increased excretion of sodium and water as well as potassium and hydrogen ions.

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Somatostatin Analogs

Class Summary

May control symptoms by suppressing secretion of gastroenteropancreatic peptides including insulin. High-dose treatment also may lead to additional antiproliferative effects. However, long-term application of somatostatin may down-regulate receptor expression levels, resulting in decreased efficiency despite increasing doses. Both short- and long-acting depot preparations are available.

Lanreotide (Somatuline Depot)

Long-acting analog of somatostatin, administered q4wk.

Octreotide acetate (Sandostatin)

Acts similarly to the natural hormone somatostatin and can suppress secretion of gastroenteropancreatic peptides, including insulin.

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Radiopharmaceuticals

Class Summary

Lutetium Lu 177-dota-tate (Lu 177), the first peptide receptor radionuclide therapy (PRRT), was approved by the FDA in January 2018. Approval was based on the NETTER-1 clinical trial. The trial was a single-institution, single-arm, open-label trial conducted by Erasmus Medical Center in Rotterdam, Netherlands in more than 1,200 patients with somatostatin receptor positive tumors. Results showed a 79% reduction in risk of disease progression or death in the Lu 177 arm compared with octreotide LAR 60 mg arm (95% CI: 0.13-0.32; p<0.0001). Median PFS was not reached in the Lu 177 arm compared with 8.5 months for octreotide LAR. An interim overall survival analysis determined that Lu 177 treatment lead to a 48% reduction in the estimated risk of death (hazard ratio 0.52, 95% CI: 0.32-0.84) compared with octreotide LAR. [45]

Lutetium Lu 177-dota-tate (Lutathera)

Binds to somatostatin receptors with highest affinity for subtype 2 receptors (SSRT2). Upon binding to somatostatin receptor-expressing cells, including malignant somatostatin receptor-positive tumors, the compound is internalized. Beta emission from Lu 177 induces cellular damage by forming free radicals in somatostatin receptor-positive cells and in neighboring cells. It is indicated for somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut neuroendocrine tumors in adults.

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Antineoplastic Agents

Class Summary

These agents inhibit cell growth and proliferation.

Streptozocin (Zanosar)

Has high affinity for neuroendocrine cells, inhibits cell proliferation, and is cytolytic. Interferes with normal function of DNA by alkylation and protein modification.

Temozolomide (Temodar)

Orally active alkylating agent; may be considered in the treatment of metastatic pancreatic neuroendocrine tumors. 

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Antineoplastic, mTOr Kinase Inhibitor

Class Summary

Mammalian target of rapamycin (mTOr), a serine-threonine kinase is dysregulated in several human cancers. Inhibitors of mTOR reduces cell proliferation, angiogenesis, and glucose uptake.

Everolimus (Afinitor)

Everolimus is indicated for progressive neuroendocrine tumors (PNET) located in the pancreas that are not surgically resectable or are metastatic. It is also indicated for well-differentiated, nonfunctional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung.

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