Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H25IN4O8 |
Molecular Weight | 560.3294 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CC[C@H](NC(=O)N[C@@H](CCCCNC(=O)NC1=CC=C([123I])C=C1)C(O)=O)C(O)=O
InChI
InChIKey=LFEGKCKGGNXWDV-NKNRFTOXSA-N
InChI=1S/C19H25IN4O8/c20-11-4-6-12(7-5-11)22-18(31)21-10-2-1-3-13(16(27)28)23-19(32)24-14(17(29)30)8-9-15(25)26/h4-7,13-14H,1-3,8-10H2,(H,25,26)(H,27,28)(H,29,30)(H2,21,22,31)(H2,23,24,32)/t13-,14-/m0/s1/i20-4
MIP-1095 I-123 is under investigation in clinical trial phase II to evaluate the safety and efficacy in combination with enzalutamide in patients with prostate-specific membrane antigen (PSMA)-avid metastatic castration-resistant prostate cancer who have progressed on abiraterone. It is known that MIP-1095 potently inhibited the glutamate carboxypeptidase activity of PSMA and when radiolabeled with 123I exhibited high affinity for prostate-specific membrane antigen (PSMA) on human prostate cancer LNCaP cells.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
(123)I-Labeled (S)-2-(3-((S)-1-carboxy-5-(3-(4-iodophenyl) ureido)pentyl)ureido)pentanedoic acid. | 2004 |
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Preclinical evaluation of novel glutamate-urea-lysine analogues that target prostate-specific membrane antigen as molecular imaging pharmaceuticals for prostate cancer. | 2009 Sep 1 |
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Repeated PSMA-targeting radioligand therapy of metastatic prostate cancer with (131)I-MIP-1095. | 2017 Jun |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT03939689
I-131-1095 will be administered intravenously at 100 mCi for the initial therapeutic dose, and up to 3 additional dose(s) between 75 mCi - 100 mCi each, administered at least 8 weeks apart as determined by initial dosimetry evaluation and occurrence of dose-limiting events.
Route of Administration:
Intravenous
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SUBSTANCE RECORD