Overview

Trade Name(s):
Lutathera
NCI Definition [1]:
A radioconjugate consisting of the tyrosine-containing somatostatin analog Tyr3-octreotate (TATE) conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential imaging and antineoplastic activities. Lutetium Lu 177-DOTA-TATE binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTR, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Tyr3-octreotate (TATE) is an octreotide derivative in which phenylalanine at position 3 is substituted by tyrosine and position 8 threoninol is replaced with threonine. SSTRs have been shown to be present in large numbers on NET and their metastases, while most other normal tissues express low levels of SSTRs.

Biomarker-Directed Therapies

Lutetium lu 177 dotatate has been investigated in 20 clinical trials, of which 18 are open and 2 are closed. Of the trials investigating lutetium lu 177 dotatate, 1 is early phase 1 (1 open), 4 are phase 1 (4 open), 3 are phase 1/phase 2 (2 open), 10 are phase 2 (9 open), 1 is phase 2/phase 3 (1 open), and 1 is phase 3 (1 open).

SSTR2 Expression, SSTR1 Expression, and SSTR3 Expression are the most frequent biomarker inclusion criteria for lutetium lu 177 dotatate clinical trials.

Adrenal gland pheochromocytoma, gastrointestinal neuroendocrine tumors, and neuroendocrine tumor are the most common diseases being investigated in lutetium lu 177 dotatate clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Lutetium Lu 177 Dotatate
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Lutetium Lu 177 Dotatate
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating lutetium lu 177 dotatate and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
lutetium lu 177-dota-tyr3-octreotate, 177 lu-dota-tyr3-octreotate, lutetium lu 177 dota(0)-tyr(3)-octreotate, dotatate lutenium lu-177, lutetium lu 177-dota-tate, lutetium lu 177-dotatate, 177 lu-dota-tyr3-octreotate, lutetium lu 177 dotatate, 177lu-dota0-tyr3-octreotate, 177 lu-dota-tate, Lutathera
Drug Target(s) [2]:
SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
NCIT ID [1]:
C95020

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.