Tagworks Pharmaceuticals BV, a Netherlands-based pioneer in Click-to-Release chemistry that promotes more effective and safer systemic therapies, has secured $65 million in Series A funding.

The investment round, which saw major participation from Spanish venture capital firm Ysios Capital and Gilde Healthcare, along with Novartis Venture Fund, New Enterprise Associates (NEA), and Lightstone Ventures, will help Tagworks Pharmaceuticals progress its lead click-cleavable Antibody-Drug Conjugate (ADC) program, TGW101.

Thomas Harth — Ysios Capital Principal said: “We are proud to have assembled such a strong, international syndicate of investors around Tagworks. Click-to-Release shows tremendous potential to bring forward a new generation of biologic therapeutics with higher efficacy and improved safety that could be very meaningful for patients.

“We look for companies with truly differentiated approaches, and thus we are delighted to support Tagworks in its next phase of development.”

Tagworks Pharmaceuticals’ TGW101 program focuses on targeting tumor-associated glycoprotein 72 (TAG72), a non-internalizing target widely prevalent in solid tumors. This ADC is designed to allow targeted and controlled drug release and activation within the tumor microenvironment, aiding in the eradication of tumors with heterogenous target expression that are challenging to treat with existing therapies.

The Dutch firm’s Click-to-Release platform enables controlled drug release through an in vivo click reaction with a trigger molecule. This has extensive applications, from expanding the scope to non-internalizing targets in ADCs for increased tumor-killing bystander effect, to on-target activation of immunomodulators and off-target deactivation of radiopharmaceuticals for improved safety and therapeutic index.

The newly secured funding will be instrumental in moving TGW101 towards initial clinical proof-of-concept and advancing the company’s broader oncology-focused pipeline. It will also allow Tagworks Pharmaceuticals, which owns a broad intellectual property estate on in vivo Click-Conjugation and Click-to-Release technology, to extend the number of ADC targets.

In addition to TGW101, Tagworks Pharmaceuticals’ pipeline includes discovery phase programs in ADCs and radiopharmaceuticals, with its technology being compatible with small molecules, peptides, larger biomolecules like antibodies and fragments, and covering various toxin and immunomodulator classes.

Marc Robillard — Tagworks Pharmaceuticals co-founder and CEO said: “Our Click-to-Release approach is poised to change the standard of care for patients with solid tumors. The limitation of today’s conventional ADCs is that they rely on suitable internalizing targets, which are not necessarily expressed by every cancer type and cancer cell.

“Our ADC therapy, however, does not depend on internalizing targets as it is based on chemically controlled release of the payload in the tumor micro-environment, thereby killing heterogenous tumors where not every cancer cell expresses the target. Accordingly, Tagworks has the potential to enhance efficacy in a safe manner through controlled payload release, and so, boost the therapeutic index.”

  Gilde Healthcare, Lightstone Ventures, Marc Robillard, Netherlands, New Enterprise Associates, Novartis Venture Fund, Tagworks Pharmaceuticals, TGW101, Thomas Harth, Ysios Capital