Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C90H120N19O35.Lu |
| Molecular Weight | 2204.9659 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 12 / 12 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[177Lu+3].CCCC[C@H](NC(=O)[C@H](CC1=CNC2=C1C=CC=C2)NC(=O)CNC(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)CN4CCN(CC([O-])=O)CCN(CC([O-])=O)CCN(CC([O-])=O)CC4)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC5=CC=CC=C5)C(N)=O
InChI
InChIKey=DTEPIUGEQLNRHF-XMGMVKEQSA-K
InChI=1S/C90H123N19O35.Lu/c1-3-4-13-56(83(137)105-66(42-75(125)126)90(144)103-63(79(91)133)39-50-10-6-5-7-11-50)97-89(143)65(41-52-43-92-55-14-9-8-12-54(52)55)96-67(111)44-93-81(135)64(40-51-15-17-53(110)18-16-51)104-80(134)49(2)94-82(136)58(20-26-70(115)116)98-85(139)60(22-28-72(119)120)100-87(141)62(24-30-74(123)124)102-88(142)61(23-29-73(121)122)101-86(140)59(21-27-71(117)118)99-84(138)57(19-25-69(113)114)95-68(112)45-106-31-33-107(46-76(127)128)35-37-109(48-78(131)132)38-36-108(34-32-106)47-77(129)130;/h5-12,14-18,43,49,56-66,92,110H,3-4,13,19-42,44-48H2,1-2H3,(H2,91,133)(H,93,135)(H,94,136)(H,95,112)(H,96,111)(H,97,143)(H,98,139)(H,99,138)(H,100,141)(H,101,140)(H,102,142)(H,103,144)(H,104,134)(H,105,137)(H,113,114)(H,115,116)(H,117,118)(H,119,120)(H,121,122)(H,123,124)(H,125,126)(H,127,128)(H,129,130)(H,131,132);/q;+3/p-3/t49-,56-,57+,58+,59+,60+,61+,62+,63-,64-,65-,66-;/m0./s1/i;1+2
| Molecular Formula | Lu |
| Molecular Weight | 176.9438 |
| Charge | 3 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C90H120N19O35 |
| Molecular Weight | 2028.0221 |
| Charge | -3 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 12 / 12 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 17:13:11 GMT 2023
by
admin
on
Sat Dec 16 17:13:11 GMT 2023
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| Record UNII |
639NVQ0SXF
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| Record Status |
Validated (UNII)
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| Record Version |
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C114499
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639NVQ0SXF
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154572874
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1771736-69-6
Created by
admin on Sat Dec 16 17:13:11 GMT 2023 , Edited by admin on Sat Dec 16 17:13:11 GMT 2023
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Official Title: 177Lu-PP-F11N for Receptor Targeted Therapy and Imaging (Theranostics) of Metastatic Medullary Thyroid Cancer - a Pilot and a Phase I Study.
Purpose: The purpose of this study is to determine the use of 177Lu-PP-F11N for imaging and therapy of patients with advanced medullary thyroid carcinoma (MTC). 177Lu-PP-F11N is a gastrin analogon, binding to cholecystokinin-2 receptors. This receptors show an overexpression on more than 90 % of medullary thyroid carcinomas.
In the pilot (phase 0) study we will correlate the tumour detection rate with the surgery and histology (proof of concept study). Furthermore, kidney protection and dosimetry studies will be performed in order to determine the kidney protection protocol and starting activity for the dose escalation study in the following, dose escalation (phase I) study. In the phase I study we will determinate the maximum tolerated dose of 177Lu-PP-F11N in patients with MTC. Furthermore, correlation with tumour radiation dose and treatment response as well as organ radiation doses and maximal tolerated dose will be performed in order to allow prospective individual patient tailored therapy planning.
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ACTIVE MOIETY |
It is the objective of the present invention to provide a gastrin analogue which show high uptake in CCK-2 receptor positive tumours by simultaneously very low accumulation in the kidneys. This objective is achieved according to the present invention by a mini-gastrin analogue PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly- Trp-Y-Asp-Phe-NH2, wherein Y stands for an amino acid replacing methionine and X stands for a chemical group attached to the peptide for the purpose of diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. In particular, very suitable compounds with respect to a high tumour to kidney ratio are mini-gastrin analogues with six D-glutamic acids or six glutamines. This so-called PP-F11N mini gastrin exhibits currently the best tumour-kidney-ratio and is therefore the most promising candidate for clinical applications.
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