Products and pipeline

Products

  • Seebri®/NVA237
  • Ultibro®/QVA149
  • NorLevo®
  • ORAVI® Mucoadhesive Tablets 50mg
    ORAVI® (Investigational Code SO-1105) is a novel formulation of the Japanese pharmacopeia miconazole (antifungal agent), the once-daily treatment mucoadhesive tablet to treat oropharyngeal candidiasis in patients.
  • *Seebri® Breezhaler®/Seebri® Inhalation Capsules 50mcg and UltibroR Breezhaler®/Ultibro® Inhalation Capsules are registered trademarks of Novartis AG.

Pipeline

Heptares Therapeutics Ltd.

Development program Target Development stage Features Partner
Muscarinic M1 receptor agonist Alzheimer's, Schizophrenia Phase I First selective muscarinic M1 receptor agonist in clinical development for treatment of Alzheimer's disease and other disorders of cognitive impairment. Currently marketed cholinesterase inhibitors require endogenous acetylcholine production and indirectly act as non-selective muscarinic agonists, resulting in both limited & transient efficacy and dose-limiting side-effects.
Muscarinic M4 receptor agonist Psychosis in schizophrenia, mental illness Phase I First-in-class selective M4 agonists for the treatment of psychosis and related behavioural & psychiatric symptoms.
Dual M1/M4 receptor agonist Psychosis and cognitive impairment in Alzheimer's, Schizophrenia and other diseases Pre-clinical First-in-class dual M1/M4 agonists for patients with co-morbid psychosis and cognitive impairment.
Adenosine A2A Cancer immuno-oncology Phase I Novel, small molecule A2A antagonist entering clinical development with additional compounds in preclinical development.
Not disclose Pain Research Drug discovery and licensing agreement with Daiichi Sankyo focused on a single G protein-coupled receptor (GPCR) nominated by Daiichi Sankyo that plays a crucial role in relieving pain.
CGRP receptor antagonist Migraine Treatment & Prophylaxis Pre-clinical Novel non-injectable small molecule antagonists of the calcitonin gene-related peptide (CGRP) receptor, a clinically validated mechanism for treating & preventing migraine attacks. Triptans contra-indicated in patients with cardiovascular disease and available prophylaxis agents have poor efficacy.
mGlu5 NAM Neurological and psychiatric disorders Pre-clinical Potential best-in-class small molecule negative allosteric modulators (NAMs) in early development.
Orexin OX1 receptor antagonist Binge Eating, Nicotine Addiction Research First selective orexin OX1 subtype receptor antagonist for treatment of addiction and compulsive disorders. OX1 antagonism is a novel mechanism to directly inhibit craving, the #1 cause of relapse in addicts, with broad applications in substance addictions (nicotine, alcohol) and compulsive disorders (binge eating, gambling).  
Orexin OX2 agonists Narcolepsy and other sleep disorders Research Orally active small molecule orexin OX2 agonists for the treatment of narcolepsy and other sleep disorders caused by diminishing orexin levels.  
Anti-PAR2 mAb Atopic dermatitis and inflammation Research Novel anti-PAR-2 antibody discovery programme.  
GLP-1 antagonist Severe hypoglycaemia, including congenital hyperinsulinism Research First-in-class, selective and orally available small molecule GLP-1 antagonists for the treatment of severe hypoglycaemia (low blood glucose) in congenital hyperinsulinism (CHI) and other hypoglycaemic conditions.  
Multiple targets (mAbs) Multiple indications Research Small molecule and antibody discovery programmes against multiple GPCR targets of with strong clinical and/or biological validation.  
Multiple targets (SMEs) Immuno-oncology Research Therapeutic antibody programmes targeting GPCR targets at key oncology checkpoints.

Partnered Development Programs

GPCR Target Indications Alliance Scope Partner
Up to 10 GPCR targets Multiple therapeutic areas Heptares will support the discovery of potential novel agents directed to the GPCR targets selected by Pfizer. Heptares is eligible to receive potential research, development, regulatory and commercial milestone payments of up to USD189 million per target.
Undisclosed CNS/pain, CV/metabolic and inflammatory disorders Approximately $190m collaboration (2011) focused on developing small molecule candidates targeting specific GPCRs.
Undisclosed Multiple indications Multi-target alliance to deliver StaR® protein as antigen for antibody discovery for selected GPCR targets.
Undisclosed Undisclosed Partnership (2012) to discover novel antibody candidates against a defined set of GPCR targets.

Related page: Heptares (StaR® technology and Structure-based drug design)

Jitsubo Co., Ltd.

NPE Target Development stage Features
JIT-8012 Gastrointestinal(GI) Research Not disclosed

Related page: Jitsubo (peptide pharmaceuticals)