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Edotreotide ( USAN, also known as (
DOTA
''Dota'' is a series of strategy video games by Valve. The series began in 2003 with the release of '' Defense of the Ancients'' (''DotA''), a fan-developed multiplayer online battle arena (MOBA) mod for the video game '' Warcraft III: Reig ...
0- Phe1- Tyr3) octreotide
Octreotide, sold under the brand name Sandostatin among others, is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was ...
, DOTA-TOC, DOTATOC) is a substance which, when bound to various radionuclides
A radionuclide (radioactive nuclide, radioisotope or radioactive isotope) is a nuclide that has excess nuclear energy, making it unstable. This excess energy can be used in one of three ways: emitted from the nucleus as gamma radiation; transferr ...
, is used in the treatment and diagnosis of certain types of cancer. When used therapeutically it is an example of peptide receptor radionuclide therapy
Peptide receptor radionuclide therapy (PRRT) is a type of radionuclide therapy, using a radiopharmaceutical that targets peptide receptors to deliver localised treatment, typically for neuroendocrine tumours (NETs).
Mechanism
A key advantage o ...
.
Yttrium-90
A phase I clinical trial ofyttrium-90
Yttrium-90 () is an isotope of yttrium. Yttrium-90 has found a wide range of uses in radiation therapy to treat some forms of cancer.
Decay
undergoes β− decay to zirconium-90 with a half-life of 64.1 hours and a decay energy of 2.28 ...
labelled edotreotide concluded in 2011, aiming to investigated effects in young cancer patients (up to 25 years of age). Specific cancers being included in the trial include neuroblastoma
Neuroblastoma (NB) is a type of cancer that forms in certain types of nerve tissue. It most frequently starts from one of the adrenal glands but can also develop in the neck, chest, abdomen, or spine. Symptoms may include bone pain, a lump i ...
, childhood brain tumours and gastrointestinal cancer.
A phase II trial
The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phase ...
for the use of 90Y DOTA-TOC for patients with metastatic
Metastasis is a pathogenic agent's spread from an initial or primary site to a different or secondary site within the host's body; the term is typically used when referring to metastasis by a cancerous tumor. The newly pathological sites, then, ...
carcinoid
A carcinoid (also carcinoid tumor) is a slow-growing type of neuroendocrine tumor originating in the cells of the neuroendocrine system. In some cases, metastasis may occur. Carcinoid tumors of the midgut ( jejunum, ileum, appendix, and cecu ...
, where octreotide
Octreotide, sold under the brand name Sandostatin among others, is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was ...
treatment was no longer effective, also reported results in 2010.
:
Lutetium-177
Lutetium-177
Naturally occurring lutetium (71Lu) is composed of one stable isotope 175Lu (97.41% natural abundance) and one long-lived radioisotope, 176Lu with a half-life of 3.78 × 1010 years (2.59% natural abundance). Thirty-five radioisotopes have been cha ...
labelled edotreotide (177Lu-DOTA-TOC), with the trade name
A trade name, trading name, or business name, is a pseudonym used by companies that do not operate under their registered company name. The term for this type of alternative name is a "fictitious" business name. Registering the fictitious name ...
Solucin, is the subject of a phase 3 clinical trial for treatment of GEP-NET
Neuroendocrine tumors (NETs) are neoplasms that arise from cells of the endocrine (hormonal) and nervous systems. They most commonly occur in the intestine, where they are often called carcinoid tumors, but they are also found in the pancreas, lung ...
s. It was granted orphan drug designation by the European Medicines Agency in 2014.
See also
*DOTA-TATE
DOTA-TATE (DOTATATE, DOTA-octreotate, oxodotreotide, DOTA-(Tyr3)-octreotate, and DOTA-0-Tyr3-Octreotate) is an eight amino acid long peptide, with a covalently bonded DOTA bifunctional chelator.
DOTA-TATE can be reacted with the radionuclides ...
, a similar compound
References
External links
* Nuclear medicine procedures Radiopharmaceuticals Somatostatin receptor agonists Macrocycles Cyclic peptides X DOTA (chelator) derivatives {{pharma-stub