Heptares Targets

GPCR Target Indication
Status Partner

Muscarinic M1 Cognitive impairment in Alzheimers, Schizophrenia, other
First-in-class selective muscarinic M1 receptor agonists in Phase 1b clinical development

Muscarinic M4 Psychosis in Schizophrenia, Alzheimer’s and other diseases
First-in-class selective M4 agonists in preclinical development

Dual M1/M4 Psychosis and cognitive impairment in Alzheimer’s, Schizophrenia and other diseases
First-in-class dual M1/M4 agonists in preclinical development

Adenosine A2A Cancer immuno-oncology
Novel, small molecule A2A antagonist (HTL1071/AZD4635) in clinical development, with additional compounds in preclinical development

CGRP Migraine
Novel, small molecule CGRP antagonists in preclinical development.

MGlu5 Neurological and psychiatric disorders
Potential best-in-class small molecule negative allosteric modulators (NAMs) in early development.

Orexin OX1 Cocaine addiction and relapse
First selective orexin OX1 receptor antagonist in preclinical development for the treatment of cocaine addiction and with potential broad applications in substance addictions (nicotine, alcohol) and compulsive disorders (binge eating, gambling).

Orexin OX2 Narcolepsy and other sleep disorders
Orally active small molecule orexin OX2 agonists for the treatment of narcolepsy and other sleep disorders caused by diminishing orexin levels.

PAR-2 Atopic dermatitis and inflammation
Novel anti-PAR-2 antibody discovery programme.

GLP-1 Severe hypoglycaemia, including congenital hyperinsulinism
First-in-class, selective and orally available small molecule GLP-1 antagonists in discovery phase

Undisclosed Immuno-oncology
Therapeutic antibody programmes targeting GPCR targets at key oncology checkpoints.

Undisclosed Multiple indications
Small molecule and antibody discovery programmes against multiple GPCR targets of with strong clinical and/or biological validation

Technology Partnerships

GPCR Target Indication
Alliance Scope Partner

Up to 10 targets Multiple indications
Small molecules and biologics discovery targeting multiple GPCRs.

Undisclosed CNS/pain,CV/metabolic and inflammatory disorders
Small molecule candidates targeting specific GPCRs.

Undisclosed Multiple indications
Novel antibody candidates against multiple GPCR targets

Undisclosed Multiple indications
Novel antibody candidates against multiple GPCR targets

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