Pharmacological Treatment of Non-Functioning Pituitary Adenomas

Vargas-Ortega, Guadalupe; Gonzalez-Virla, Baldomero; Romero-Gameros, Carlos Alfonso

doi:10.1016/j.arcmed.2023.102917

Cited by 1 publication

(1 citation statement)

References 55 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…They are not associated with 2 of 10 clinical evidence of hormonal hypersecretion, but patients present neurological symptoms such as headache and visual field defects due to the mass effect and clinical signs of pituitary hormone deficiencies [1][2][3]. The first-line treatment is transsphenoidal surgery, but recurrences are frequent and additional treatment is needed in the vast majority of patients [4][5][6]. However, no effective medical therapy is available for NF-PitNETs.…”

Section: Introductionmentioning

confidence: 99%

The Novel SSTR3 Agonist ITF2984 Exerts Antimitotic and Proapoptotic Effects in Human Non-Functioning Pituitary Neuroendocrine Tumor (NF-PitNET) Cells

Di Muro,

Catalano,

Treppiedi

et al. 2024

IJMS

View full text Add to dashboard Cite

Somatostatin receptor ligands (SRLs) with high affinity for somatostatin receptors 2 and 5 (SSTR2 and SSTR5) are poorly efficacious in NF-PitNETs, expressing high levels of SSTR3. ITF2984 is a pan-SSTR ligand with high affinity for SSTR3, able to induce SSTR3 activation and to exert antitumoral activity in the MENX rat model. The aim of this study was to test ITF2984’s antiproliferative and proapoptotic effects in NF-PitNET primary cultured cells derived from surgically removed human tumors and to characterize their SSTR expression profile. We treated cells derived from 23 NF-PitNETs with ITF2984, and a subset of them with octreotide, pasireotide (SRLs with high affinity for SSTR2 or 5, respectively), or cabergoline (DRD2 agonist) and we measured cell proliferation and apoptosis. SSTR3, SSTR2, and SSTR5 expression in tumor tissues was analyzed by qRT-PCR and Western blot. We demonstrated that ITF2984 reduced cell proliferation (−40.8 (17.08)%, p < 0.001 vs. basal, n = 19 NF-PitNETs) and increased cell apoptosis (+41.4 (22.1)%, p < 0.001 vs. basal, n = 17 NF-PitNETs) in all tumors tested, whereas the other drugs were only effective in some tumors. In our model, SSTR3 expression levels did not correlate with ITF2984 antiproliferative nor proapoptotic effects. In conclusion, our data support a possible use of ITF2984 in the pharmacological treatment of NF-PitNET.

show abstract