rodatristat (KAR 5417) / Sumitomo Pharma - LARVOL DELTA

A Study of Rodatristat Ethyl in Patients With Pulmonary Arterial Hypertension (ELEVATE 2) (clinicaltrials.gov) - P2; N=90; Recruiting; Sponsor: Altavant Sciences GmbH; Not yet recruiting ➔ Recruiting

Enrollment open • Hypertension • Pulmonary Arterial Hypertension • Respiratory Diseases • 5-Hydroxyindoleacetic Acid

[VIRTUAL] ELEVATE 2: A multicenter study of rodatristat ethyl in patients with WHO Group 1 pulmonary arterial hypertension (PAH) (ERS 2021) - P2 | "RE alone was more effective in reducing pulmonary vascular remodeling induced by SUGEN hypoxia than tadalafil + ambrisentan. RE, with its novel MoA distinct from those of approved therapies, has potential to be a new treatment option for PAH patients."

Clinical • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

Pharmacokinetics and Excretion of Oral [14C]-Rodatristat Ethyl (clinicaltrials.gov) - P1; N=6; Not yet recruiting; Sponsor: Altavant Sciences GmbH

New P1 trial

A Study of Rodatristat Ethyl in Patients With Pulmonary Arterial Hypertension (ELEVATE 2) Estudio de Rodatristat de etilo en pacientes con hipertensión arterial pulmonar (ELEVATE 2) (clinicaltrialsregister.eu) - P2; N=90; Ongoing; Sponsor: Altavant Sciences GmbH

New P2 trial • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Rare Diseases • Respiratory Diseases

[VIRTUAL] A Pharmacokinetic/Pharmacodynamic Based Rationale for Dose Selection of the TPH Inhibitor Rodatristat Ethyl in ELEVATE-2 - a Phase 2b Study in Pulmonary Arterial Hypertension (ATS 2021) - "Simulations indicate that 300 mg and 600mg BID RE may have a high probability of lowering serotonin biosynthesis to extents associated with vascular remodeling and reductions in pulmonary vascular resistance in rat models of PAH and have the potential to improve exercise capacity over the 24-week treatment period of ELEVATE-2."

P2b data • PK/PD data • Congestive Heart Failure • Heart Failure • Hypertension • Pulmonary Arterial Hypertension • Respiratory Diseases • 5-Hydroxyindoleacetic Acid

[VIRTUAL] Serotonin Pathobiology in Pulmonary Arterial Hypertension and Phase 2b Investigation of the Novel Therapy Rodatristat Ethyl (RE) in WHO Group 1 PAH (ATS 2021) - "Sponsored by Altavant Sciences This program will include an expert overview of the role serotonin plays in the pathogenesis of PAH, present the mode of action of rodatristat ethyl; a novel inhibitor of peripheral serotonin via targeting of tryptophan hydroxylase 1, and provide an overview of the phase 2b clinical program, ELEVATE 2"

P2b data • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

A Study of Rodatristat Ethyl in Patients With Pulmonary Arterial Hypertension (ELEVATE 2) (clinicaltrials.gov) - P2; N=90; Not yet recruiting; Sponsor: Altavant Sciences GmbH

Clinical • New P2 trial • Hypertension • Pulmonary Arterial Hypertension • Respiratory Diseases

[VIRTUAL] Tissue Distribution and Biomarker Data for Rodatristat, A Novel Serotonin Synthesis Inhibitor for PAH, Demonstrate Negligible Blood-Brain Barrier Penetration and Pharmacologically Meaningful Exposure in Lung (ATS-I 2020) - P2a | "Tissue distribution and biomarker data support the lack of impact on brain 5-HT in rat. In lung, free drug exceeded the TPH1 IC 50 and lowered 5-HT in PAH rats. Data support low risk of human CNS effects and further development of rodatristat in PAH."

Biomarker • Hypertension • Pulmonary Arterial Hypertension • 5-Hydroxyindoleacetic Acid

Tissue Distribution and Biomarker Data for Rodatristat, A Novel Serotonin Synthesis Inhibitor for PAH, Demonstrate Negligible Blood-Brain Barrier Penetration and Pharmacologically Meaningful Exposure in Lung (ATS 2020) - P2a | "Tissue distribution and biomarker data support the lack of impact on brain 5-HT in rat. In lung, free drug exceeded the TPH1 IC50 and lowered 5-HT in PAH rats. Data support low risk of human CNS effects and further development of rodatristat in PAH."

Biomarker • 5-Hydroxyindoleacetic Acid

A Study of RVT-1201 in Patients With Pulmonary Arterial Hypertension (ELEVATE 1) (clinicaltrials.gov) - P2a; N=3; Terminated; Sponsor: Altavant Sciences GmbH; N=36 ➔ 3; Recruiting ➔ Terminated; Inability to enroll

Clinical • Enrollment change • Trial termination

Safety, tolerability, pharmacokinetics and pharmacodynamics after repeated once or twice daily RVT-1201, a TPH inhibitor for treatment of PAH (ERS 2019) - "RVT-1201, in development for PAH, is a pro-drug for the metabolically-stable TPH inhibitor KAR5417... Once or twice daily RVT-1201 was generally well tolerated and achieved meaningful reductions in serotonin biosynthesis supporting progression to Phase 2 studies in PAH."

Clinical • PK/PD data