Delving into the Latest Updates on Iofolastat (123I) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug, Diagnostic radiopharmaceuticals

Synonyms

IOFOLASTAT I 123(USAN), 123I-MIP-1072, MIP-1072

+ [1]

Target

PSMA

Mechanism

PSMA inhibitors(Prostate-specific membrane antigen inhibitors), SPECT(Single-photon emission-computed tomography enhancers)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication-

Inactive Indication

Metastatic Prostate Carcinoma

Originator Organization

Molecular Insight Pharmaceuticals, Inc.

Active Organization-

Inactive Organization

Molecular Insight Pharmaceuticals, Inc.

Drug Highest PhasePendingPhase 1

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC19H26IN3O7

InChIKeyOXUUJYOSVPMNKP-ZANJDRPYSA-N

CAS Registry949575-24-0

This is an open-label study comparing the imaging characteristics of 123-I-MIP-1072 and ProstaScint® (111-In-capromab pendetide)in patients with metastatic prostate cancer. Eligible patients will receive a dose of 123-I-MIP-1072 and have imaging studies and safety assessments (physical examination, vital signs, electrocardiogram, clinical laboratory tests) performed during the subsequent 24 hours. Two weeks later, patients will return for additional safety assessments and will receive ProstaScint® if they don't already have a pre-existing ProstaScint scan. Final assessments will be performed two weeks after the ProstaScint® scan unless there is a difference between the 123-I-MIP-1072 and ProstaScint® scans. If this is the case, another dose of 123-I-MIP-1072 will be given 12 weeks later, and imaging studies repeated.

Start Date01 Oct 2009

Sponsor / Collaborator

Molecular Insight Pharmaceuticals, Inc.

NCT00712829

/ CompletedPhase 1

A Phase I Study Evaluating the Safety, Pharmacokinetics, Tissue Distribution, Metabolism of Small Molecule Inhibitors of Prostate Specific Membrane Antigen: Determination of I-123 Radiation Dosimetry for 123-I-MIP-1072 and 123-I-MIP-1095

This is a single blinded, randomized, cross-over design. Up to 12 patients will be randomly administered a single 10.0 mCi dose of 123I-MIP-1072 or 123I-MIP-1095 (study drugs). The second (alternate) study drug will be administered approximately 14 days after the first. A final follow-up visit will occur approximately 2 weeks after the injection of the alternate study drug.

Start Date01 May 2008

Sponsor / Collaborator

Molecular Insight Pharmaceuticals, Inc.

100 Clinical Results associated with Iofolastat (123I)

Login to view more data

100 Translational Medicine associated with Iofolastat (123I)

Login to view more data

100 Patents (Medical) associated with Iofolastat (123I)

Login to view more data

10

Literatures (Medical) associated with Iofolastat (123I)

01 May 2018·Bioorganic & medicinal chemistryQ3 · MEDICINE

Development of a Ga-68 labeled PET tracer with short linker for prostate-specific membrane antigen (PSMA) targeting

Q3 · MEDICINE

Article

Author: Moon, Sung-Hyun ; Kim, Young Ju ; Chung, June-Key ; Hong, Mee Kyung ; Lee, Yun-Sang ; Lee, Dong Soo ; Jeong, Jae Min

Glu-Urea-Lys (GUL) derivatives have been reported as prostate-specific membrane antigen (PSMA) agent. We developed derivatives of GUL conjugated with NOTA or DOTA via a thiourea linker and tested their feasibility as PSMA imaging agents after labeling with ⁶⁸Ga. NOTA-GUL and DOTA-GUL were synthesized and labeled with ⁶⁸Ga using generator-eluted ⁶⁸GaCl₃ in 0.1 M HCl in the presence of 1 M NaOAc at pH 5.5. The stabilities of ⁶⁸Ga-labeled compounds in human serum were tested at 37.5 °C. A competitive binding assay was performed using the PSMA-positive prostate cancer cell line 22Rv1 and [¹²⁵I]MIP-1072 (PSMA-specific binding agent) as a tracer. Biodistribution and micro-PET studies were performed using 22Rv1-xenograft BALB/c nude mice. The radiolabeling efficiency of NOTA-GUL (>99%) was higher than that of DOTA-GUL (92%). The IC₅₀ of Ga-NOTA-GUL was 18.3 nM. In the biodistribution study, tumor uptake of ⁶⁸Ga-NOTA-GUL (5.40% ID/g) was higher than that of ⁶⁸Ga-DOTA-GUL (4.66% ID/g) at 1 h. Tumor/muscle and tumor/blood uptake ratios of ⁶⁸Ga-NOTA-GUL (31.8 and 135, respectively) were significantly higher than those of ⁶⁸Ga-DOTA-GUL (16.1 and 31.1, respectively). The tumor/kidney uptake ratio of ⁶⁸Ga-NOTA-GUL was 3.4-fold higher than that of ⁶⁸Ga-DOTA-GUL. ⁶⁸Ga-NOTA-GUL showed specific uptake to PSMA positive tumor xenograft and was blocked by co-injection of the cold ligand. In conclusion, we successfully synthesized ⁶⁸Ga-NOTA-GUL and ⁶⁸Ga-DOTA-GUL for prostate cancer imaging. ⁶⁸Ga-NOTA-GUL showed better radiochemical and biodistribution results. ⁶⁸Ga-NOTA-GUL may be a promising PSMA targeting radiopharmaceutical.

01 Oct 2016·Journal of nuclear medicine : official publication, Society of Nuclear MedicineQ1 · MEDICINE

The Rise of PSMA Ligands for Diagnosis and Therapy of Prostate Cancer

Q1 · MEDICINE

Review

Author: Kopka, Klaus ; Babich, John W ; Giesel, Frederik L ; Haberkorn, Uwe ; Eisenhut, Michael ; Kratochwil, Clemens ; Afshar-Oromieh, Ali

The prostate-specific membrane antigen (PSMA) has received increased consideration during the past few years as an excellent target for both imaging and therapy of prostate cancer. After many years of outstanding preclinical research, the first significant step forward in clinical use was achieved in 2008 with the first human experience with the small-molecule PSMA inhibitors ¹²³I-MIP-1972 and ¹²³I-MIP-1095. A clinical breakthrough followed in 2011 with ⁶⁸Ga-PSMA-11 for PET imaging and ¹³¹I-MIP-1095 for endoradiotherapy of metastatic prostate cancer. Since then, PET/CT with ⁶⁸Ga-PSMA-11 has rapidly spread worldwide, and endoradiotherapy with PSMA ligands has been conducted at increasing numbers of centers. ⁶⁸Ga-PSMA-11 is currently the subject of multicenter studies in different countries. Since 2013, ¹³¹I-related PSMA therapy has been replaced by ¹⁷⁷Lu-labeled ligands, such as PSMA-617, which is also the subject of multicenter studies. Alternative PSMA ligands for both imaging and therapy are available. Among them is ^99mTc-MIP-1404, which has recently entered a phase 3 clinical trial. This article focuses on the highlights of the development and clinical application of PSMA ligands.

01 May 2016·Nanomedicine : nanotechnology, biology, and medicineQ2 · MEDICINE

Development of a complementary PET/MR dual-modal imaging probe for targeting prostate-specific membrane antigen (PSMA)

Q2 · MEDICINE

Article

Author: Chung, June-Key ; Moon, Sung-Hyun ; Kim, Young Ju ; Lee, Yun-Sang ; Yang, Bo Yeun ; Hong, Mee Kyung ; Lee, Dong Soo ; Jeong, Jae Min

FROM THE CLINICAL EDITOR:

The combination of using Positron Emission Tomography (PET) and computed tomography (CT) in clinical practice is now the norm. With advances in technology, the next step would be to develop combined PET and Magnetic Resonance (MR) dual-imaging. In this article, the authors described their positive study on the development of a dual-modal PET/MR imaging probe using a prostate cancer model.

100 Deals associated with Iofolastat (123I)

Login to view more data