Kainova Therapeutics

Science built for impact

Our breakthrough GPCR-modulating therapies in immuno-oncology and inflammation create new possibilities.

Patients deserve more than hope

We deliver therapies that change outcomes where options are limited.

Our GPCR expertise is unrivalled

Together with our validated drug discovery and development approach, they enable differentiated therapies to target unmet needs.

We drive a diversified pipeline

Our CCR8, PAR2 and EP4 targeting candidates have clear patient relevance and therapeutic promise.

Changing what we can expect from medicine

By showing patients and partners that better is always possible.

About Us

At Kainova Therapeutics, our work is driven by one pivotal question: how can science deliver better outcomes for patients with underserved medical needs? The answer is rooted in our commitment to bold science, to collaboration, and to patients who need new treatment options.

We focus on breakthrough GPCR-modulating therapies in immuno-oncology and inflammation, built on decades of scientific and medical expertise from our leadership team, and our proprietary, validated approach. We foster a culture where scientific excellence and human purpose go hand in hand.

We measure success not only by advancing uniquely differentiated clinical assets, but by the depth of our science, the strength of our team, and the relevance of our therapies to patients’ lives. With first-in-class and best-in-class programs, we aim to redefine standards of care and create lasting value for patients, partners, and investors.

Our growing portfolio of assets

Asset Disc Discovery Pre-IND Pre-IND Ph1 Phase 1 Ph2 Phase 2
DT-9081 EP4 Receptor Antagonist
Solid Tumors
Phase 1
DT-7012 Anti-CCR8 Depleting Antibody
Solid Tumors
Phase 1
DT-9046 PAR2 Biased Antagonist
Inflammation
Pre-IND
Undisclosed GPCR Targets
Discovery

DT-9081 EP4 Receptor Antagonist

  • Discovery
  • Pre-IND
  • Phase 1
  • Phase 2

DT-9081: an EP4R antagonist overcoming PGE2-mediated immunosuppression

DT-9081, a Phase II-ready EP4 receptor (EP4R) antagonist, represents a breakthrough potential in anti cancer therapeutics. This oral small molecule is designed to reverse the immunosuppressive effects of Prostaglandin E2 (PGE2) produced by the COX-2 positive tumors. By reversing PGE2-mediated immunosuppression, DT-9081 aims at restoring an immunocompetent microenvironment, enabling immune reactivation and driving tumor regression in different solid cancer indications.

DT-9081 was evaluated in the EPRAD study, an open-label, multicenter Phase I trial in patients with advanced, recurrent or metastatic solid tumors. For more details, please visit clinicaltrials.gov/study/NCT05582850.

DT-9081: our translational research and precision science in action

In preclinical studies, DT-9081 has shown significant antitumor effects in multiple animal models (sarcoma, colorectal or breast cancer) when combined with immune checkpoint inhibitors (ICIs) such as anti-PD1, anti-CTLA4, and/or chemotherapies. Such combo dramatically induced or increased the number of complete responders vs monotherapy or SOC.

Leveraging comprehensive tumor biology and deep GPCR pharmacology expertise, our team has established a robust biomarker strategy. These biomarkers inform clinical positioning and enable precise monitoring of EP4 receptor engagement during treatment, helping de-risk development and ensure efficient, informative clinical trial strategy. By sharpening patient stratification and enhancing trial design, Kainova Therapeutics aims to strengthen clinical trial development and ultimately improve outcomes for patients.

Reversing GPCR-mediated immunosuppression to optimize anticancer treatments

Although several current antitumor therapies, including chemotherapy and certain ICIs, can be effective, immune resistance is often observed, associated with a boost of PGE2 secretion by cancer cells, leading to immunosuppressive environment and tumor development, and resulting in poor prognosis for patients.

Targeting the COX-2/PGE2/EP4 axis with selective EP4 receptor antagonism is a potent novel therapeutic strategy applicable to several tumor types. This approach restores cancer recognition by the immune system, overcomes immunotherapy resistance and optimizes the efficacy of anticancer treatments.

Combining DT-9081 with anticancer therapies, with the aim of boosting the immune system, could lead to more sustainable and potent treatments, extending innovative treatment options for cancer patients.

DT-7012 Anti-CCR8 Depleting Antibody

  • Discovery
  • Pre-IND
  • Phase 1
  • Phase 2

DT-7012: a best-in-class Treg-depleting anti-CCR8 antibody pioneering a new era in GPCR-targeting immunotherapies

DT-7012, a Phase I/II differentiated anti-CCR8 monoclonal antibody, represents a breakthrough in GPCR-targeting cancer immunotherapies. It is designed to selectively deplete highly immunosuppressive regulatory T cells (Tregs) via antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP) mechanisms. This action restores immune competence within the tumor microenvironment (TME), aiming at promoting tumor regression and opening new possibilities for patients who have not responded to existing immunotherapies.

First patients have been dosed in the DOMISOL Phase I / II clinical trial, an open-label, multicenter study, evaluating safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary anti-tumor activity of DT-7012 in patients with resistant and advanced solid tumors. For more details, please visit clinicaltrials.gov NCT06819735.

DT-7012 benefits from multiple and strong patent protection, highlighting the broad therapeutic application of our Treg-depleting ADCC/ADCP antibodies and reinforcing our leadership in GPCR-targeting immunotherapy.

DT-7012: transformative immunotherapy with unique differentiating properties

Our deep CCR8 pharmacology expertise and translational research strategy underpin DT-7012’s development. A unique collection of proprietary anti-CCR8 antibodies combined to a rigorous benchmarking against leading CCR8 antibodies led to DT-7012 standing out as best-in-class.

By selectively depleting highly suppressive CCR8+ Tregs, DT-7012 amplifies the activity of immunocompetent cells such as Dendritic cells, NK cells and CD8 T cells, improving the overall immune response against tumors. Unlike the majority of other anti-CCR8 clinical candidates, DT-7012 targets broader forms of the CCR8 receptor presenting post-translational modifications, thereby extending its therapeutic potential to a wider range of immunosuppressive Treg subpopulations.

Another standout feature of DT-7012 is its ability to prevent CCL1 ligand-induced CCR8 internalization, a critical factor for Treg depletion. By ensuring CCR8 remains at the membrane, DT-7012 potentiates depletion mechanisms, even in challenging CCL1-rich tumor microenvironments. This sustained Treg depletion is essential for effective cancer immunotherapy, conferring breakthrough therapeutic properties to this program.

CCR8: a superior target for Treg depletion, unlocking the cancer-fighting abilities of the immune system

CCR8 is a member of the GPCR family and has been shown to be predominantly expressed by highly immunosuppressive regulatory Tregs.

While immune-checkpoint inhibitors (ICI) have revolutionized cancer treatment, the tumor-infiltrating Tregs suppress immune response in TME, driving resistance against ICIs and compromising the efficacy of these treatments.

Strategic depletion of Tregs via CCR8 is a highly promising approach to counter immunoresistance in the TME. DT-7012 is at the forefront of this innovative approach, unlocking the immune system’s cancer-fighting abilities and offering a powerful new therapeutic solution that can transform the lives of cancer patients worldwide.

DT-9046 PAR2 Biased Antagonist

  • Discovery
  • Pre-IND
  • Phase 1
  • Phase 2

DT-9046: a first-in-class biased antagonist of PAR2 transforming treatment for inflammatory diseases

DT-9046, a highly differentiated first-in-class and pre-IND biased negative allosteric modulator (NAM) of Proteinase-Activated Receptors 2 (PAR2) is a potent, orally available small molecule designed to selectively modulate the T helper type 2 (Th2) immune responses. By addressing the root causes of multiple inflammatory diseases, such as atopic dermatitis (AD), inflammatory bowel disease (IBD), arthritis and pain, DT-9046 offers a bold new therapeutic option for patients with limited choices today.

Progressing through pre-IND studies with a solid data package, DT-9046 stands out for its differentiated mechanism of action. Unlike biologics and orthosteric antagonist-based approach, DT-9046 delivers unique advantages such as unsurmountability, sustained drug’s blocking activity even under high endogenous ligand levels and acidic conditions. Its biased ligand design enables an optimal modulation of PAR2 signalling, minimizing the risk of resistance while maintaining efficacy.

Backed by strong patent protection, DT-9046 reflects Kainova Therapeutics’ commitment to delivering a diversified pipeline of transformative therapies that address critical patient needs.

Advancing GPCR-targeting therapeutics: Redefining PAR2 antagonism

Current treatments for inflammatory diseases often fall short due to immune escape or treatment resistance. PAR2, long considered one of the most challenging GPCR targets, has eluded effective therapeutic solutions within the pharmaceutical industry. Leveraging Kainova’s deep expertise in targeting complex GPCRs, DT-9046 provides the potential of a differentiated multimodal approach, that could offer patients safer, more effective solutions for inflammatory diseases.

Undisclosed GPCR Targets

  • Discovery
  • Pre-IND
  • Phase 1
  • Phase 2

Kainova Therapeutics is advancing a portfolio of G protein-coupled receptors (GPCRs) targets that represent breakthrough opportunities in immuno-oncology and inflammation. These receptors sit at the core of mechanisms driving immunomodulation, therapeutic resistance, and chronic disease, yet remain largely untapped by existing therapies.

Through our proprietary platform and integrated drug discovery and development approach, we have identified and de-risked novel GPCR targets with the potential to deliver first-in-class and best-in-class therapies. Our programs span both small molecules and larger biological molecules, expanding a differentiated pipeline built to address areas of high unmet need.

In recent years, GPCRs such as CCR8 but also A2aR, A2bR and EP4R have emerged as high potential targets in immuno-oncology, given their central roles in mediating immunosuppression and resistance to checkpoint inhibitors. These receptors offer powerful entry points for next-generation therapies designed to reshape the tumor microenvironment and improve anti-tumor immunity.

On the inflammation side, GPCRs remain underexplored but equally critical. PAR2 receptor is known for decades for its unique ability to fine-tune immune and inflammatory responses, barrier integrity, and pain. However, it has proven exceptionally difficult for the pharmaceutical industry to drug effectively. Kainova’s approach leverages allosteric modulation to precisely tune PAR2 function via biased small molecule ligands , offering a promising path forward for this complex receptor.

By pursuing challenging and high-value targets, Kainova Therapeutics strengthens its competitive advantage while demonstrating the breath and ambition of its innovation.

Our main partnerships

  • Logo for Merck
  • Logo for Pfizer
  • Logo for Bristol Myers Squibb
  • Logo for Université de Montréal
  • Logo for Condor
  • Logo for RHU Sprint

A team of passionate and
success-driven leaders

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Newsroom

Recents News

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Feature

Image for Kainova <br /> Introduction

Kainova
Introduction


Our Chief Executive Officer, Sean A. MacDonald, shares insights about our company and purpose.