MELBOURNE, Australia I July 18, 2023 I Telix Pharmaceuticals Limited (ASX: TLX, Telix, the Company) today announces that the first patient has been dosed in a Phase I study of the Company’s investigational targeted radiation therapy, TLX250, in combination with a Merck KGaA, Darmstadt, Germany (Merck) DNA-dependent protein kinase (DNA-PK) inhibitor candidate, peposertib (M3814). The study is being conducted in patients with solid tumours expressing carbonic-anhydrase IX (CAIX), a potential pan-cancer target.

STARSTRUCK ( Identifier: NCT05868174) is a Phase Ib, open label, single-arm, multicentre dose escalation and dose expansion study to evaluate the safety profile, dosing and activity of TLX250 (177Lu-DOTA-girentuximab) in combination with the DNA damage response inhibitor (DDRi) peposertib, which is an inhibitor of DNA-PK. The target population is patients with CAIX-expressing solid tumours that are relapsed or refractory to standard therapies. Up to 80 patients will be assessed in this study in Australian sites.

The clinical hypothesis is that the combination of TLX250 and a DNA-PK inhibitor provides an enhancement in potency through their synergistic action on cancer cells. Targeted radiation effectively induces DNA damage in targeted cancer cells and the DNA-PK inhibitor may act to prevent the cell from repairing this damage, resulting in higher potency at lower doses. This hypothesis was confirmed in preclinical studies, conducted under a strategic research collaboration between Merck and Telix announced in 2019,[1] and provided evidence that the combined effect of Merck’s investigational DNA-PK inhibitor peposertib with Telix’s targeted radiation candidate has potential to significantly improve efficacy and reduce the required radiation dose for tumour reduction and remission, compared to targeted radiation alone.

Principal Investigator for the STARSTRUCK study, Professor Nat Lenzo, GenesisCare Group Clinical Director Theranostics said, “The treatment of advanced cancer can be extremely challenging. We are pleased to support the commencement of this study with Telix to help determine if there is a potential future clinical benefit regarding the combination of molecular targeted radiation and DNA-PK inhibitors.”

Telix Chief Medical Officer, Dr. Colin Hayward stated, “Preclinical data has shown excellent combination response, which has potential to translate to additional response or more tolerable treatment regimens in patients. We would like to thank Prof. Lenzo and his clinical team at GenesisCare Murdoch, as well as the patients who will contribute to this important study.”

Merck and Telix are continuing the initial scientific collaboration to further explore and optimise the combination of TLX250 or other next-generation targeted radiation therapy candidates with Merck’s DDRi compounds in preclinical studies.

About TLX250

TLX250 (177Lu-DOTA-girentuximab) is an antibody-based therapeutic platform that targets CAIX, a cell surface protein that is highly expressed in several human cancers, and is currently the subject of the STARLITE-1 ( Identifier: NCT05663710) and STARLITE-2 (NCT05239533) studies in combination with immunotherapy.[2] High CAIX tumour expression is generally correlated with poor prognosis.

Telix’s companion investigational diagnostic imaging agent TLX250-CDx (89Zr-DFO-girentuximab) was the subject of a successful global Phase III trial (ZIRCON trial, NCT03849118), which completed enrolment and reported positive top-line data during 2022.[3] Analyses of primary endpoints and key secondary endpoints of the ZIRCON trial were presented to the medical community for the first time at ASCO GU on 18 February 2023.[4] TLX250-CDx is currently being investigated in the Phase II STARBURST study ( Identifier: NCT05563272) exploring CAIX expression in patients with a diverse range of solid tumours for potential diagnostic and therapeutic applications.[5]

About Telix Pharmaceuticals Limited

Telix is a biopharmaceutical company focused on the development and commercialisation of diagnostic and therapeutic radiopharmaceuticals. Telix is headquartered in Melbourne, Australia with international operations in the United States, Europe (Belgium and Switzerland), and Japan. Telix is developing a portfolio of clinical-stage products that aims to address significant unmet medical need in oncology and rare diseases. Telix is listed on the Australian Securities Exchange (ASX: TLX).

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TLX250 and TLX250-CDx have not received a marketing authorisation in any jurisdiction. Telix’s lead product, Illuccix® (gallium-68 (68Ga) gozetotide (also known as 68Ga PSMA-11) injection), has been approved by the U.S. Food and Drug Administration (FDA),[6] and by the Australian Therapeutic Goods Administration (TGA),[7] and by Health Canada.[8] Telix is also progressing marketing authorisation applications for this investigational candidate in the United Kingdom and the European Union.[9]

[1] Telix ASX disclosure 1 August 2019.

[2] Telix ASX disclosure 14 September 2021.

[3] Telix ASX disclosure 7 November 2022.

[4] Telix media release 20 February 2023.

[5] Telix media release 19 June 2023.

[6] Telix ASX disclosure 20 December 2021.

[7] Telix ASX disclosure 2 November 2021.

[8] Telix ASX disclosure 14 October 2022.

[9] Telix ASX disclosure 3 April 2023.

SOURCE: Telix Pharmaceuticals