In-house Programs

Our emerging pipeline of in-house programs comprises drug candidates advancing through various stages of early development and preclinical studies with a focus on core therapeutic areas including neurology, gastro-intestinal, inflammatory and other indications. Our plan is to advance only the highest quality programs from our proprietary pipeline to clinical development, with the intent to eventually commercialize selected products in designated markets ourselves.

PHASE 3

Daridorexant

INDICATION: Insomnia

MODALITY: Small molecule

WHOLLY-OWNED BY:


Daridorexant is a dual orexin receptor antagonist (DORA) that blocks the binding and activity of the wake-promoting neuropeptides known as orexins. In October 2022, daridorexant achieved positive Phase 3 top-line results in Japanese patients with insomnia. This successful trial paves the way for a potential regulatory submission in Japan in H2 2023. Daridorexant is approved in the U.S. and Europe and marketed in these territories under the brand name QUVIVIQ™ by Idorsia. Sosei Heptares has the Japanese and APAC (ex-China) rights for daridorexant.

 

+ Press Release

Oct 31, 2023: Sosei Heptares Announces Submission of New Drug Application in Japan for Daridorexant (ACT-541468), a Dual Orexin Receptor Antagonist for the Treatment of Insomnia

 

 

 

 

 

Ph1/2a

EP4 antagonist

CANDIDATE: HTL0039732

INDICATION: Immuno-oncology

MODALITY: Small molecule

WHOLLY-OWNED BY:


Sosei Heptares is advancing a novel, highly selective and potent antagonist of the EP4 receptor to mediate PGE2 immunosuppression in the tumor microenvironment within oncology. 

In July 2022, Sosei Heptares and Cancer Research UK signed an agreement to bring Sosei Heptares’ cancer immunotherapy drug candidate into a first-in-human trial.Under the Clinical Trial and Licence Agreement (CTLA), Cancer Research UK’s Centre for Drug Development will sponsor, design and execute a Phase I/IIa clinical trial of HTL0039732, a novel selective EP4 antagonist.

Sosei Heptares will be responsible for CTA enabling activities, including GLP toxicology, IMP manufacture1 and other necessary pre-clinical studies in preparation for the opening of the clinical trial. Sosei Heptares holds a licence to the results generated under the trial to continue the clinical development and commercialisation of HTL0039732. 

 

+ Clinical Trials

 

+ Press Releases

Preclinical

Muscarinic M1 agonist (Japan)

CANDIDATE: Undisclosed

INDICATION: Neurology

MODALITY: Small molecule

WHOLLY-OWNED BY:


In November 2021, Sosei Heptares and Neurocrine Biosciences, Inc. enter the 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.

Under the terms of the agreement, Neurocrine Biosciences gains development and commercialization rights to a broad portfolio of novel clinical and preclinical subtype-selective muscarinic M4, M1 and dual M1/M4 receptor agonists discovered by Sosei Heptares in development for the treatment of major neurological disorders. 

Sosei Heptares retains the rights to develop M1 agonists in Japan in all indications, with Neurocrine Biosciences receiving co-development and profit share options.

 

+ Press Releases

Preclinical

EP4 agonist

INDICATION: Inflammatory bowel disease

MODALITY: Small molecule

WHOLLY-OWNED BY:


Sosei Heptares is developing an oral small molecule EP4 agonist for the treatment of Inflammatory bowel disease. PTGER4 has been identified as a candidate susceptibility gene for IBD and plays a critical role in maintaining barrier homeostasis. An EP4 agonist is anticipated to bring clinical benefit by improving mucosal healing. Our lead molecule is a novel gut restricted EP4 agonist that has shown robust efficacy across a range of preclinical models.

Discovery

SARS-CoV-2 MPro

CANDIDATE: SH-879

INDICATION: Coronaviruses

MODALITY: Small molecule

WHOLLY-OWNED BY:


In April 2020, we initiated an R&D program focused on the design and development of novel drugs targeting the SARS-CoV-2 coronaviruses and to treat COVID-19. We have applied our structure-based drug design capabilities and cutting-edge technologies to precision-design new inhibitors of the SARS-CoV-2 MPro protease, which plays a crucial role in viral replication.

Potential clinical candidates have now been identified, suitable for further development. MPro inhibitor SH-879 represents an excellent opportunity for further development as an oral drug for the treatment of COVID-19:

  • Shows comparable antiviral activity to Pfizer’s oral candidate PF-07321332 against SARS-CoV-2 in cell based assays;
  • Has low in vitro clearance, superior in vivo clearance and high plasma exposure from oral dosing critically important to inhibit the virus.
  • Does not likely require co-dosing with ritonavir for PK boosting in human clinical trials, differentiating from Pfizer’s PF-07321332

+ Press Releases

+ Factsheet

Pre-discovery and Discovery Programs