Novel Myc inhibitor to be tested in early-phase cancer clinical trial

The Spanish Agency of Medicines and Medical Devices has approved the first-in-human phase I/II clinical trial of Myc-inhibiting compound Omomyc (OMO-103) in patients with advanced solid tumours. This is an important step towards creating a clinically viable and direct inhibitor of Myc, a protein that’s associated with the formation of most tumour types.

This milestone builds on preclinical proof of the efficacy and safety of the cell-penetrating Omomyc polypeptide in mouse models. It also follows the successful development of anti-Myc peptides for treating several different types of tumour, achieved with support from the EU-funded project SYST-iMYC. The company responsible for developing the disruptive Myc-inhibitor is Peptomyc, a spin-off born from the Vall d’Hebron Institute of Oncology (VHIO) that hosted the SYST-iMYC project.

“We have previously shown that Myc blockade has an excellent therapeutic effect in several mouse models, with mild side effects that are well tolerated and reversible,” reports VHIO Mouse Models of Cancer Therapies Group lead researcher Laura Soucek in a news item posted on the VHIO website. “Now that we have received approval to initiate our early phase clinical trial, we can further progress in testing the safety and efficacy of our Omomyc-based therapy for the benefit of those who matter the most – our patients,” continues Soucek, who is also the co-founder and CEO of Peptomyc.Myc regulates many biological processes, such as ribosome biogenesis and metabolism. In most tumour types, Myc activity is deregulated, which contributes to the progression and maintenance of the disease. This makes the protein a promising target for anticancer drugs. However, for many years scientists have believed that Myc is undruggable, mainly because of the potentially catastrophic side effects in normal tissues. With the approval to trial their Myc inhibitor in selected Spanish clinics, the Peptomyc team is now proving these naysayers wrong.

“At the preclinical level, we have reported the efficacy of Omomyc as a cell penetrating peptide – essentially, a mini-protein with the ability to enter cells and reach its target compartment, namely, the nucleus. The successful intravenous systemic administration of our mini-protein MYC inhibitor against lung cancer and other malignancies, has led to this week’s exciting development,” notes Peptomyc co-founder and Chief Scientific Officer Marie-Eve Beaulieu in the same news item, dated 17 March 2021.

The team’s strategy is very different from previous approaches to inhibiting Myc. “Our Omomyc mini-protein is large enough to accurately fold and adapt to Myc’s disordered structure, which determines the specificity of inhibition. At the same time, it is small enough to penetrate tumor cells and nuclei in order to reach its target,” Beaulieu goes on to explain. “By conducting our first-in-human early phase clinical trial, we hope to drive this novel therapy into the clinic for the more effective treatment of multiple tumor types.”

Peptomyc will soon start treating patients with Omomyc in three clinical trial sites in Barcelona and Madrid. Twenty cancer patients with advanced solid tumours whose disease has progressed after previous treatments will be enrolled in the phase I study. The SYST-iMYC (Development of an effective and safe systemic Myc inhibitor for the treatment of multiple cancer types.) project that contributed to this achievement ended in December 2019.

For more information, please see:

SYST-iMYC project