SAR-bisPSMA - Next-Generation, Highly Targeted Prostate Cancer Theranostic

SAR-bisPSMA combines the well characterised PSMA peptide, which has been in many thousands of patients to date, with Clarity’s proprietary SAR Technology and the theranostic isotopes of copper.

SAR-bisPSMA Clinical Trial Overview

Study name	Products	Indication	Phase	Number of Patients	Location	Status	Reference
	⁶⁴Cu SAR-bisPSMA	Prostate diagnostic	I	30	AUS	Study objectives reached	NCT04839367
	⁶⁴SAR-bisPSMA/ ⁶⁷SAR-bisPSMA	Prostate therapy	I/IIa	34	USA	Recruiting	NCT04868604
	⁶⁴Cu SAR-bisPSMA	Prostate diagnostic	I/II	50	USA	Recruiting	NCT05249127

^64/67Cu SAR-bisPSMA:
A Next-Generation PSMA theranostic

SAR-bisPSMA is a next generation theranostic which combines two PSMA binding motifs linked to Clarity’s SAR chelator technology, allowing the identical molecule to be used for diagnostic (via Cu-64) and therapeutic applications (via Cu-67).

Comparison of % injected activity in tumour in the same preclinical model (LNCAP) for PSMA-617 and SAR-bisPSMA

SAR-bisPSMA is potentially the best in class theranostic agent for prostate cancer and has demonstrated superior uptake in tumour at 1 and 24 hours compared to PSMA-617.

Comparison of % Injected Activity/g in tumour of
SAR-bisPSMA to PSMA-617

SAR-bisPSMA has the ideal product characteristics for a radiopharmaceutical

⁶⁴Cu-SAR-bisPSMA demonstrated fast uptake and retention in tumours as well as rapid clearance from normal organs in preclinical models.

⁶⁴Cu-SAR-bisPSMA

⁶⁷Cu-SAR-bisPSMA

Zia et al., 2019. Ang.Chem

McInnes et al., 2020. JNM

Fast uptake and retention in tumours

Biodistribution in a LNCaP xenograft model of ⁶⁴Cu SAR-bisPSMA showing high uptake and retention in tumours as well as rapid clearance from key organs over 24 hours

Rapid kidney clearance of unbound product

Positron Emission Tomography images showing ⁶⁴Cu SAR-bisPSMA targeting to tumours within 1 hour and otherwise rapid kidney clearance

Significant anti-tumour effect

Xenograft mice with LNCaP tumours were injected with a single or repeat dose of up to 30 MBq of ⁶⁷Cu SAR-bisPSMA.

About prostate cancer

Prostate cancer is the second most common cancer in men and the 5^th leading cause of death in men worldwide.

Patients diagnosed with prostate cancer at later stages have poor treatment outcomes, indicating a high unmet need for early detection and better treatment options for metastatic castration-resistant prostate cancer.

About PSMA

PSMA is a protein expressed in all types of prostatic tissue and is an excellent diagnostic and therapeutic target. Targeted molecular imaging using PSMA increases detection of metastatic sites and is steering clinical options for late-stage prostate cancer management.