Pasireotide: a novel treatment for patients with acromegaly
Daniel Cuevas-Ramos,1 Maria Fleseriu2,3 1Department of Endocrinology and Metabolism, Neuroendocrinology Clinic, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán, Mexico City, Mexico; 2Department of Medicine (Endocrinology), 3Department of Neurolog...
| Main Authors: | , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Dove Medical Press
2016-01-01
|
| Series: | Drug Design, Development and Therapy |
| Subjects: | |
| Online Access: | https://www.dovepress.com/pasireotide-a-novel-treatment-for-patients-with-acromegaly-peer-reviewed-article-DDDT |
| _version_ | 1818558698278092800 |
|---|---|
| author | Cuevas-Ramos D Fleseriu M |
| author_facet | Cuevas-Ramos D Fleseriu M |
| author_sort | Cuevas-Ramos D |
| collection | DOAJ |
| description | Daniel Cuevas-Ramos,1 Maria Fleseriu2,3 1Department of Endocrinology and Metabolism, Neuroendocrinology Clinic, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán, Mexico City, Mexico; 2Department of Medicine (Endocrinology), 3Department of Neurological Surgery, Northwest Pituitary Center, Oregon Health & Science University, Portland, OR, USA Abstract: Morbidity and mortality rates in patients with active acromegaly are higher than the general population. Adequate biochemical control restores mortality to normal rates. Now, medical therapy has an increasingly important role in the treatment of patients with acromegaly. Somatostatin receptor ligands (SRLs) are considered the standard medical therapy, either after surgery or as a first-line therapy when surgery is deemed ineffective or is contraindicated. Overall, octreotide and lanreotide are first-generation SRLs and are effective in ~20%–70% of patients. Pegvisomant, a growth hormone receptor antagonist, controls insulin-like growth factor 1 in 65%–90% of cases. Consequently, a subset of patients (nonresponders) requires other treatment options. Drug combination therapy offers the potential for more efficacious disease control. However, the development of new medical therapies remains essential. Here, emphasis is placed on new medical therapies to control acromegaly. There is a focus on pasireotide long-acting release (LAR) (Signifor LAR®), which was approved in 2014 by the US Food and Drug Administration and the European Medicine Agency for the treatment of acromegaly. Pasireotide LAR is a long-acting somatostatin multireceptor ligand. In a Phase III clinical trial in patients with acromegaly (naïve to medical therapy or uncontrolled on a maximum dose of first-generation SRLs), 40 and 60 mg of intramuscular pasireotide LAR achieved better biochemical disease control than octreotide LAR, and tumor shrinkage was noted in both pasireotide groups. Pasireotide LAR tolerability was similar to other SRLs, except for a greater frequency and degree of hyperglycemia and diabetes mellitus. Baseline glucose may predict hyperglycemia occurrence after treatment, and careful monitoring of glycemic status and appropriate treatment is required. A precise definition of patients with acromegaly who will derive the greatest therapeutic benefit from pasireotide LAR remains to be established. Lastly, novel therapies and new potential delivery modalities (oral octreotide) are summarized. Keywords: pasireotide, somatostatin analogs, emerging treatments, growth hormone, insulin-like growth factor 1, somatostatin receptor ligand |
| first_indexed | 2024-12-14T00:15:42Z |
| format | Article |
| id | doaj.art-3e47605f05144e4eb342c76e5b403e87 |
| institution | Directory Open Access Journal |
| issn | 1177-8881 |
| language | English |
| last_indexed | 2024-12-14T00:15:42Z |
| publishDate | 2016-01-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Drug Design, Development and Therapy |
| spelling | doaj.art-3e47605f05144e4eb342c76e5b403e872022-12-21T23:25:32ZengDove Medical PressDrug Design, Development and Therapy1177-88812016-01-012016Issue 122723925181Pasireotide: a novel treatment for patients with acromegalyCuevas-Ramos DFleseriu MDaniel Cuevas-Ramos,1 Maria Fleseriu2,3 1Department of Endocrinology and Metabolism, Neuroendocrinology Clinic, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán, Mexico City, Mexico; 2Department of Medicine (Endocrinology), 3Department of Neurological Surgery, Northwest Pituitary Center, Oregon Health & Science University, Portland, OR, USA Abstract: Morbidity and mortality rates in patients with active acromegaly are higher than the general population. Adequate biochemical control restores mortality to normal rates. Now, medical therapy has an increasingly important role in the treatment of patients with acromegaly. Somatostatin receptor ligands (SRLs) are considered the standard medical therapy, either after surgery or as a first-line therapy when surgery is deemed ineffective or is contraindicated. Overall, octreotide and lanreotide are first-generation SRLs and are effective in ~20%–70% of patients. Pegvisomant, a growth hormone receptor antagonist, controls insulin-like growth factor 1 in 65%–90% of cases. Consequently, a subset of patients (nonresponders) requires other treatment options. Drug combination therapy offers the potential for more efficacious disease control. However, the development of new medical therapies remains essential. Here, emphasis is placed on new medical therapies to control acromegaly. There is a focus on pasireotide long-acting release (LAR) (Signifor LAR®), which was approved in 2014 by the US Food and Drug Administration and the European Medicine Agency for the treatment of acromegaly. Pasireotide LAR is a long-acting somatostatin multireceptor ligand. In a Phase III clinical trial in patients with acromegaly (naïve to medical therapy or uncontrolled on a maximum dose of first-generation SRLs), 40 and 60 mg of intramuscular pasireotide LAR achieved better biochemical disease control than octreotide LAR, and tumor shrinkage was noted in both pasireotide groups. Pasireotide LAR tolerability was similar to other SRLs, except for a greater frequency and degree of hyperglycemia and diabetes mellitus. Baseline glucose may predict hyperglycemia occurrence after treatment, and careful monitoring of glycemic status and appropriate treatment is required. A precise definition of patients with acromegaly who will derive the greatest therapeutic benefit from pasireotide LAR remains to be established. Lastly, novel therapies and new potential delivery modalities (oral octreotide) are summarized. Keywords: pasireotide, somatostatin analogs, emerging treatments, growth hormone, insulin-like growth factor 1, somatostatin receptor ligandhttps://www.dovepress.com/pasireotide-a-novel-treatment-for-patients-with-acromegaly-peer-reviewed-article-DDDTpasireotideacromegalygrowth hormoneinsulin-like growth factor 1somatostatin receptor ligand |
| spellingShingle | Cuevas-Ramos D Fleseriu M Pasireotide: a novel treatment for patients with acromegaly Drug Design, Development and Therapy pasireotide acromegaly growth hormone insulin-like growth factor 1 somatostatin receptor ligand |
| title | Pasireotide: a novel treatment for patients with acromegaly |
| title_full | Pasireotide: a novel treatment for patients with acromegaly |
| title_fullStr | Pasireotide: a novel treatment for patients with acromegaly |
| title_full_unstemmed | Pasireotide: a novel treatment for patients with acromegaly |
| title_short | Pasireotide: a novel treatment for patients with acromegaly |
| title_sort | pasireotide a novel treatment for patients with acromegaly |
| topic | pasireotide acromegaly growth hormone insulin-like growth factor 1 somatostatin receptor ligand |
| url | https://www.dovepress.com/pasireotide-a-novel-treatment-for-patients-with-acromegaly-peer-reviewed-article-DDDT |
| work_keys_str_mv | AT cuevasramosd pasireotideanoveltreatmentforpatientswithacromegaly AT fleserium pasireotideanoveltreatmentforpatientswithacromegaly |