NeuroEndocrine Tumor Therapy with Lutetium-177-octreotate and Everolimus (NETTLE): A Phase I Study

Abstract

In combination, PRRT with (177)Lu-octreotate, the maximum tolerated dose of everolimus is 7.5 mg daily.

Radiopeptides for Imaging and Therapy: A Radiant Future

“…Moreover, the physical properties of 18 F are more favorable for PET imaging than those of 68 Ga. Indeed, an 18 F-labeled GRPR antagonist, BAY 864367 (3-cyano-4-18 F-fluorobenzoyl-Ala(SO 3 H)-Ala(SO 3 H)-Ava-Gln-Trp-Ala-ValNMeGly-His-Sta-Leu-NH 2 ), has recently been implemented in the clinical setting (4).…”

“…Indeed, an 18 F-labeled GRPR antagonist, BAY 864367 (3-cyano-4-18 F-fluorobenzoyl-Ala(SO 3 H)-Ala(SO 3 H)-Ava-Gln-Trp-Ala-ValNMeGly-His-Sta-Leu-NH 2 ), has recently been implemented in the clinical setting (4). A drawback yet to be overcome with 18 Flabeled peptides is their higher lipophilicity, which gives rise to less favorable pharmacokinetics. An interesting approach consists of labeling peptides with Al 18 F via radiometalation chemistry.…”

“…Several peptides have been labeled with Al 18 F, such as octreotide, E[c(RGDyK)] 2 , exendin-4, the bombesin analog NOTA-8-Aoc-BBN(7-14)NH 2 , and the GRPR antagonist JMV4168 (DOTA-bAla-bAla-JMV594) (7,8). The development of a kit-based method for labeling peptides with 18 F would make application of 18 F-labeled peptides possible in a wider range of hospitals.…”

“…Capecitabine and temozolomide both increased the response rate of 177 Lu-DOTATATE in comparison with 177 Lu-DOTATATE alone (17). A recent proof-of-concept study described the combination of PRRT with everolimus (18). It was shown that everolimus can safely be combined with 177 Lu-octreotate to treat low-grade NETs.…”

“…Radiopeptides have established themselves as important agents for imaging, but also for PRRT. For medical imaging, peptides can be radiolabeled with radionuclides such as 99m Tc, 111 In, 67 Ga, or 123 I for SPECT and 18 F, 68 Ga, 64 Cu, 86 Y, or 124 I for PET. For therapeutic purposes, peptides can be labeled with b-emitters such as 177 Lu, 90 Y, or 67 Cu and a-emitters such as 213 Bi or 225 Ac.…”