Partnered Programs

Our partnered pipeline includes drug candidates that we have out-licensed to leading pharmaceutical and biotechnology companies, including AstraZeneca and AbbVie; and drug candidates for which we have ongoing single or multi-target discovery and development collaborations, including with AbbVie, BiohavenGenentech, GSK, Takeda, and Pfizer. Our partners are developing one or more drug candidates that we discovered using our SBDD platform. We believe these strategic partnerships validate our GPCR technologies and SBDD platform capabilities, and also provide a diversified source of revenues in the form of up-front and milestone payments.

Our partnered pipeline also includes drug candidates that we are currently co-developing, or which we plan to co-develop, with collaboration partners under profit and risk-sharing arrangements. We have entered into strategic co-development agreements with Kymab and PeptiDream, for the discovery, development and commercialization of certain novel antibody therapeutics and peptides.

Partnered GPCR Pipeline Programs (Out-licensed)

PHASE 2

Adenosine A2a antagonist

CANDIDATE: AZD4635 / imaradenant

INDICATION: mCRPC

MODALITY: Small molecule

PARTNER:


AZD4635 is a novel, potent, small molecule, adenosine A2a receptor antagonist discovered by us and licensed to AstraZeneca in 2015. The blockade of adenosine production in the tumor micro-environment is quickly emerging as one of the leading immuno-oncology treatment approaches and AZD4635 is one of the most advanced A2a receptor antagonists under investigation.

AZD4635 is in a Phase 2 clinical trial for patients with metastatic castration resistant prostate cancer (mCRPC). The first arm of the clinical trial will investigate AZD4635 with AstraZeneca’s PD-L1 antibody durvalumab (Imfinzi®). The second arm of the clinical trial will investigate AZD4635 with Imifinzi® and Cabazitaxel.

AZD4635 is also being investigated in an ongoing Phase 1 clinic study in patients with Advanced Solid Malignancies.

AZD4635 has been designed to have a low molecular weight, good solubility and attractive drug-like properties coupled with high potency and selectivity, allowing it to be given at very high doses required to overcome the local high concentrations of adenosine.

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PHASE 1

GLP-1 agonist

CANDIDATE: PF-07081532

INDICATION: T2DM / Obesity

MODALITY: Small molecule

PARTNER:


Sosei Heptares and Pfizer initiated a strategic drug discovery collaboration in 2015 to research and develop potential new medicines directed at up to 10 GPCR targets nominated by Pfizer in multiple therapeutic areas. The nominated targets have strong clinical and biological validation as key points for therapeutic intervention in their respective diseases but have proved very challenging to address with conventional discovery approaches, with sub-optimal or no medicines approved to date.

Since the start of the collaboration we have delivered multiple preclinical milestones, including StaR®s, X-ray structures and lead molecules, as well as new intellectual property. In December 2019, Sosei Heptares was notified by Pfizer that it has dosed the first subject in a clinical trial with a new drug candidate nominated from the multi-target drug discovery collaboration between the two companies.

+ Press Releases

PHASE1

CCR6 antagonist

CANDIDATE: PF-07054894

INDICATION: Inflammatory bowel disease

MODALITY: Small molecule

PARTNER:


Sosei Heptares and Pfizer initiated a strategic drug discovery collaboration in 2015 to research and develop potential new medicines directed at up to 10 GPCR targets nominated by Pfizer in multiple therapeutic areas. The nominated targets have strong clinical and biological validation as key points for therapeutic intervention in their respective diseases but have proved very challenging to address with conventional discovery approaches, with sub-optimal or no medicines approved to date.

Since the start of the collaboration we have delivered multiple preclinical milestones, including StaR®s, X-ray structures and lead molecules, as well as new intellectual property. 

+ Press Releases

Preclinical

Pfizer Collaboration

INDICATION: Metabolic and other diseases

MODALITY: Small molecule

PARTNER:


Sosei Heptares and Pfizer initiated a strategic drug discovery collaboration in 2015 to research and develop potential new medicines directed at up to 10 GPCR targets nominated by Pfizer in multiple therapeutic areas. The nominated targets have strong clinical and biological validation as key points for therapeutic intervention in their respective diseases but have proved very challenging to address with conventional discovery approaches, with sub-optimal or no medicines approved to date.

Since the start of the collaboration we have delivered multiple preclinical milestones, including StaR®s, X-ray structures and lead molecules, as well as new intellectual property. 

+ Press Releases

Preclinical

GPR35 agonist

INDICATION: Inflammatory bowel disease/GI disorders

MODALITY: Small molecule

PARTNER:


Sosei Heptares entered into a global collaboration and license agreement with GlaxoSmithKline (“GSK”) in 2020. The single-target agreement is focused on the discovery and development of selective, oral, small molecule agonists of GPR35, an important orphan G protein-coupled receptor (GPCR) with genetic association to inflammatory bowel disease (IBD) and other gastrointestinal immune disorders, for which there remains significant unmet need for millions of sufferers worldwide.

 

+ Press Releases

Discovery

Pfizer Collaboration

INDICATION: Multiple therapeutic areas

MODALITY: Small molecule and monoclonal antibody

PARTNER:


Sosei Heptares and Pfizer initiated a strategic drug discovery collaboration in 2015 to research and develop potential new medicines directed at up to 10 GPCR targets nominated by Pfizer in multiple therapeutic areas. The nominated targets have strong clinical and biological validation as key points for therapeutic intervention in their respective diseases but have proved very challenging to address with conventional discovery approaches, with sub-optimal or no medicines approved to date.

Since the start of the collaboration we have delivered multiple preclinical milestones, including StaR®s, X-ray structures and lead molecules, as well as new intellectual property. 

+ Press Releases

Discovery

Genentech Collaboration

INDICATION: Multiple therapeutic areas

MODALITY: Small molecule and/or biologic

PARTNER:


Sosei Heptares announced a multi-target research collaboration and license agreement with Genentech, a member of the Roche Group, in 2019 to discover and develop novel medicines (new small molecules and/or biologics) that modulate multiple GPCR targets of interest to Genentech. The nominated targets represent promising new therapeutic intervention points across a range of diseases.

+ Press Releases

Discovery

Takeda Collaboration

INDICATION: Gastrointestinal diseases and other therapeutic areas

MODALITY: Small molecule and/or biologic

PARTNER:


Sosei Heptares announced a strategic multi-target partnership with Takeda in 2019 to discover, develop and commercialize novel molecules, including small molecules and biologics, that modulate GPCR targets of interest to Takeda. The nominated targets represent new therapeutic intervention points across a range of diseases. The collaboration will initially focus on high-priority gastrointestinal targets, but the agreement includes the potential expansion into other therapeutic areas.

+ Press Releases

Discovery

AbbVie Collaboration

INDICATION: Inflammatory and Autoimmune Diseases

MODALITY: Small molecule

PARTNER:


Sosei Heptares announced an exclusive discovery collaboration and option to license agreement with AbbVie in June 2020 to discover, develop and commercialize novel medicines that modulate GPCR targets of interest to AbbVie. The collaboration will initially focus on discovery of novel small molecules targeting inflammatory and autoimmune diseases.

+ Press Releases

Partnered GPCR Pipeline Programs (Profit share/Co-development)

Preclinical

CXCR4 mAb

CANDIDATE: KY1051

INDICATION: Immuno-oncology

MODALITY: Monoclonal antibody

PARTNER:


In 2016, Sosei Heptares Group and Kymab entered into a strategic collaboration to discover, develop and commercialize novel antibody therapeutics targeting a number of GPCRs with an initial focus on immuno-oncology. KY1051 CXCR-4 product candidate is the first program governed by the terms of the Collaboration Agreement.

GPCRs are widely expressed on cells of the innate and adaptive immune system and play key roles in modulating cell migration and recruitment to the tumor environment, activation, survival, proliferation and differentiation. GPCRs act at critical checkpoints that can be targeted by novel immunotherapy antibodies.

Under the agreement, we will apply our StaR® platform to create stable antigens based on multiple GPCR targets chosen by the companies. Kymab will then use its IntelliSelect™ Transgenic platform to generate antibodies in response to immunization with these antigens. Promising leads will be progressed using the partners’ complementary skills, resources and development capabilities in order to bring innovative products into the clinic. Under the agreement, the companies will jointly conduct and share the costs of each antibody discovery and development program.

KY1051 is an antibody that binds CXCR4, a chemokine receptor that plays a key role in modulating the immune system and the tumour microenvironment. KY1051 neutralizes the binding of CXCR4 to its ligand CXCL12, which we believe will allow treatment in combination with immune-checkpoint therapies in a wide range of malignancies.

+ Press Releases

Discovery

PAR2 Peptide

INDICATION: Inflammation

MODALITY: Peptide

PARTNER:


In 2017, Sosei Heptares Group and PeptiDream entered into a strategic collaboration to discover, develop and commercialize novel therapeutics targeting Protease activated receptor 2 (PAR2), a GPCR that plays an important role in inflammatory diseases.

The collaboration brings together two drug discovery platforms and preclinical and clinical development capabilities. We will apply our StaR® platform and resulting 3D structural insights to the GPCR target selected by both companies. PeptiDream will use its proprietary Peptide Discovery Platform System (PDPS) technology to identify macrocyclic/constrained peptides against the target GPCR and to optimize hit peptides and/or small molecules for further development. Promising leads will be progressed using the partners’ complementary skills, resources and development capabilities in order to bring innovative products into the clinic. Under the agreement, the companies will jointly conduct and share the costs of the discovery and development program and will co-own any resulting products.

+ Press Releases

Discovery

Targeted GPCR Degradation

INDICATION: Gastrointestinal disorders

MODALITY: Small molecule

PARTNER:


In 2020, Sosei Heptares and Captor Therapeutics SA (Captor) entered a strategic technology collaboration focused on the discovery and development of novel small molecules that target the degradation of disease-associated G protein-coupled receptors (GPCRs). Targeted protein degradation (TPD) is an approach whereby the body’s natural process for degrading proteins is diverted using small molecule drugs to eliminate disease-causing proteins.
The selective destruction of such proteins is expected to have multiple advantages over classical drugs such as inhibitors and antibodies for the development of novel therapeutics against a broad range of diseases.

+ Press Releases

Discovery

AI Augmented Drug Discovery

INDICATION: Neurology diseases

MODALITY: Small molecule

PARTNER:


In January 2021, Sosei Group Corporation and PharmEnable, a UK drug discovery company, entered a collaboration to apply their respective technologies to drive novel drug discovery against a challenging G protein-couple receptor (GPCR) target associated with neurological diseases.

The collaboration will combine Sosei Heptares’ world-leading GPCR-focused structure-based drug design platform, which has fully structurally enabled the GPCR target, providing detailed structural insights and an assessment of tractability, with PharmEnable’s proprietary advanced artificial intelligence (AI)-enabled and medicinal chemistry technologies (ChemUniverse and ChemSeek) to identify novel, highly specific drug leads for further development.

PharmEnable’s approach identifies three-dimensional (3D) drug candidate hits with improved specificity compared with traditional screening methods and allows the company to take on particularly challenging biological targets, such as “peptidergic” GPCRs, which have proved difficult to drug using existing approaches.

+ Press Releases

 

Discovery

Ion Channels

INDICATION: Neurology diseases

MODALITY: Small molecule

PARTNER:


February 2021– Sosei Heptares announced it will apply its world-leading structure-based drug design (SBDD) expertise and platform to ion channels for the first time through a new strategic collaboration with Metrion Biosciences Limited (“Metrion”), the specialist ion channel CRO and drug discovery company.

Ion channels are a class of integral membrane proteins that regulate the flow of ions across the cell membrane as a means of conducting signals between cells and their environment. They are well established drug targets, particularly in neurological and cardiovascular diseases, but many remain undrugged or poorly drugged, and may be tractable to structure-based approaches.

The collaboration aims to demonstrate the potential of Sosei Heptares’ SBDD technologies to address disease-associated ion channels and work towards establishing a leadership position in this area, in a similar way that it has done for G protein-coupled receptors (GPCRs).

As a first step, Sosei Heptares and Metrion will combine their respective capabilities in a drug discovery program to identify novel, highly specific drug leads for further development against a single ion channel associated with neurological diseases.

+ Press Releases

Asset-centric Companies

PHASE 1

mGlu5 NAM

CANDIDATE: HTL0014242

INDICATION: Substance use disorders

MODALITY: Small molecule

COMPANY:


HTL0014242 is a potent and selective mGlu5 small molecule negative-allosteric modulator (NAM) discovered by us as a potential treatment for certain neurological orders. 

On November 2020 Sosei Group Corporation entered into an agreement with Tempero Bio, under which Tempero Bio has in-licensed exclusive global rights to Sosei Heptares’ mGlu5 negative allosteric modulator (NAM) program to develop therapies targeting substance use disorders and anxiety. Tempero Bio is a new company created by Aditum Bio in collaboration with Sosei Heptares to develop the mGlu5 NAM program, including the candidate HTL0014242. Tempero Bio will be funded by Aditum Bio.

Under the terms of the agreement, Tempero Bio will obtain exclusive global rights to a portfolio of potent, orally available metabotropic glutamate receptor 5 (mGlu5) NAM modulators, including HTL0014242, which were precision-designed by Sosei Heptares using its GPCR Structure-Based Drug Design (SBDD) platform. The candidate HTL0014242 will be renamed TMP-301.

+ Press Releases

+ Publications

Discovery

Orexin agonists

INDICATION: Narcolepsy

MODALITY: Small molecule

COMPANY:


Orexia Therapeutics is developing oral and intranasal orexin receptor agonists under two discovery programs using structure-based drug design approaches. These agonists target the treatment of narcolepsy type 1, where they have the potential to directly address the underlying pathology of orexin neuron loss, as well as other neurological disorders characterized by excessive daytime sleepiness.

Orexia Therapeutics is a subsidiary of Centessa Pharmaceuticals, a novel asset-centric pharmaceutical company designed and built to advance a portfolio of highly validated programs.

+ Press Releases