Partnered Programs

Our partnered pipeline includes clinical candidates identified by Heptares using the SBDD platform and  out-licensed to leading pharmaceutical and biotechnology companies, including GSK and Neurocrine, for further development; and drug candidates that were identified and are being developed by other companies under single or multi-target discovery and development collaborations, including with AbbVie, Genentech, Takeda and Pfizer. We believe these strategic partnerships and technology collaborations 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. 

Out-licensing Collaborations

PHASE 1

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. 

+ Clinical Trials

+ Press Releases

PHASE 1

MC4 antagonist

CANDIDATE: PF-07258669

INDICATION: Anorexia

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

PHASE 1

GLP-1 agonist

CANDIDATE: PF-06954522

INDICATION: metabolic 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

PHASE 2

Muscarinic M4 agonist

CANDIDATE: NBI-1117568 (HTL0016878)

INDICATION: Schizophrenia and other neuropsychiatric disorders

MODALITY: Small molecule

PARTNER:


HTL0016878 is a first-in-class, selective and orally available, small molecule muscarinic M4 receptor agonist being advanced through clinical development as a potential new treatment for neurobehavioural symptoms associated with Alzheimer’s disease. HTL0016878 has been designed to work through a different mechanism of action than available antipsychotics. The high selectivity of HTL0016878 offers the possibility for an improved safety profile over previous non-selective muscarinic receptor agonists.

In January 2021, Sosei Heptares had regained the worldwide rights to its muscarinic agonist programs.

In November 2021, Neurocrine Biosciences, Inc. and Sosei Group Corporation entered into a strategic collaboration and licensing agreement to develop novel muscarinic receptor agonists, which Neurocrine Biosciences intends to study in the treatment for schizophrenia, dementia and other neuropsychiatric disorders. Transaction completion expected by 31 December 2021.

+ Clinical Trials

+ Press Releases

PHASE 1

Muscarinic M4 preferring agonist

CANDIDATE: NBI-1117569

INDICATION: Neurology diseases

MODALITY: Small molecule

PARTNER:


NBI-1117569, a muscarinic M1-preferring agonist, is investigational, oral compounds, which may have the potential to treat neurological and neuropsychiatric conditions and were developed utilizing Sosei Heptares' structure-based drug design platform.

 

+ Press Releases

PHASE 1

Dual Muscarinic M1/M4 agonists

CANDIDATE: NBI-1117570

INDICATION: Major CNS disorders

MODALITY: Small molecule

PARTNER:


In the collaboration with AbbVie (formerly Allergan), we advanced a series of selective, small molecule, dual M1/M4 agonists through preclinical development. Such molecules have the potential to treat both cognitive impairment and neurobehavioral symptoms associated with Alzheimer’s disease and other neurological diseases.

In January 2021, Sosei Heptares had regained the worldwide rights to its muscarinic agonist programs from AbbVie.

In November 2021, Neurocrine Biosciences, Inc. and Sosei Group Corporation entered into a strategic collaboration and licensing agreement to develop novel muscarinic receptor agonists, which Neurocrine Biosciences intends to study in the treatment for schizophrenia, dementia and other neuropsychiatric disorders. Transaction completion expected by 31 December 2021.

 

+ Press Releases

Preclinical

Muscarinic M1 preferring agonist

CANDIDATE: NBI-1117567

INDICATION: Neurology diseases

MODALITY: Small molecule

PARTNER:


NBI-1117567, a muscarinic M1-preferring agonist, is investigational, oral compounds, which may have the potential to treat neurological and neuropsychiatric conditions and were developed utilizing Sosei Heptares' structure-based drug design platform. Neurocrine confirmed a Phase 1 study of NBI-1117567 will be initiated in 2024.

+ Press Releases

PHASE 1

GPR52 agonist

CANDIDATE: HTL0048149

INDICATION: Schizophrenia

MODALITY: Small molecule

PARTNER:


GPR52 is an orphan G protein-coupled receptor (GPCR) highly expressed in the brain, especially in the striatum and the prefrontal cortex, and represents a potential emerging therapeutic target for a range of neurological and neuropsychiatric disorders. We have developed a portfolio of selective GPR52 agonists and modulators leveraging proprietary insights from its StaR® technology SBDD platform, the most advanced of which (HTL0048149) entered in a first-in-human clinical trial in 202310.

+ Press Releases

 

Preclinical

GSK4381406

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.

+ Clinical Trials

+ 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

Discovery

Lilly Collaboration

CANDIDATE: Undisclosed

INDICATION: Diabetes Metabolic

MODALITY: Small molecule

PARTNER:


In December 2022, Sosei Heptares has entered a drug discovery collaboration with Eli Lilly and Company, a global biopharmaceutical company, to discover, develop and commercialize small molecules that modulate novel G protein-coupled receptor (GPCR) targets associated with diabetes and metabolic diseases. 

This new agreement will leverage Sosei Heptares’ StaR® technology and structure-based drug design (SBDD) platform and Lilly’s extensive drug development and commercialization expertise as well as its therapeutic area expertise in diabetes and metabolic diseases. 

Under the terms of the agreement, Sosei Heptares will focus its efforts on multiple GPCR targets nominated by Lilly to deliver novel target-selective small molecule hit candidates for further development and commercialization. Sosei Heptares receives an upfront payment of US$37 million on signing and is eligible to receive development and commercial milestones totalling up to US$694 million, plus tiered royalties on global sales.

+ Press Releases

Co-development / Profit-share Collaborations

Preclinical

CXCR4 mAb

CANDIDATE: KY1051

INDICATION: Immuno-oncology

MODALITY: Monoclonal antibody

PARTNER:


In 2016, Sosei Heptares Group and Kymab (currently known as Sanofi) 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 (currently Sanofi)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.

Sanofi announced in April, 2021 the successful completion of its acquisition of Kymab Group Ltd., adding KY1005 to its pipeline, a fully human monoclonal antibody targeting key immune system regulator OX40L.

+ 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

AI Augmented Drug Discovery

INDICATION: Immune diseases

MODALITY: Small molecule

PARTNER:


In July 2021, Sosei Heptares and InveniAI,a global leader in pioneering the application of artificial intelligence (AI) and machine learning (ML) to transform innovation across drug discovery and development, announced the initiation of a new R&D collaboration.

The objective of the collaboration is to identify new therapeutic product concepts for immune diseases where an AI and ML based approach can be applied to generate compelling evidence for the role of G-protein coupled receptors (GPCRs) in relevant immunomodulatory pathways; the goal being to use these targets as a basis for SBDD to generate novel compounds that could improve responses to existing immunotherapies.

+ Press Releases

Discovery

Gut-brain axis drug discovery

CANDIDATE: Undisclosed

INDICATION: Gastrointestinal disorders

MODALITY: Small molecule

PARTNER:


In May 2022, Sosei Heptares and New York City-based Kallyope, pioneers in drug discovery involving the gut-brain axis, have entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR) targets with a goal of creating new drug discovery programs in the area of gastrointestinal diseases. 

The agreement will leverage Sosei Heptares’ GPCR Diversified Compound Library and GPCR expertise with the innovative Kallyope gut-brain axis platform, which combines single-cell sequencing, circuit mapping, computational biology and enteroid phenotypic screening. Together, the companies will prioritize and validate GPCR drug targets that represent new opportunities for potential therapeutic intervention in gastrointestinal diseases and create programs for the development of novel small molecules that modulate these targets. 

+ Press Releases

Discovery

AI Augmented Drug Discovery

INDICATION: Immune-mediated diseases

MODALITY: Small molecule

PARTNER:


In January 2022, Sosei Heptares entered into a research collaboration with Verily to combine Verily's Immune Profiler and Sosei Heptares' StaR®  platform to generate novel drug candidates against GPCR targets for immune-mediated diseases.

Verily’s proprietary Immune Profiler is a next generation immune mapping platform that combines high-resolution molecular phenotyping performed in Verily’s labs and advanced computational analysis techniques to generate insights into immune system functions. It will be used to identify GPCR targets that represent new opportunities to modulate immune cell function and ameliorate disease pathology.

 

+ Press Releases

Co-owned investments

PHASE 1

mGlu5 NAM

CANDIDATE: HTL0014242 (TMP-301)

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

Preclinical

OX2 agonist (Oral)

CANDIDATE: ORX750

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