TMP-301 / Nxera Pharma, Tempero Bio - LARVOL DELTA

TMP-301-AUD-201: A Study to Investigate the Safety and Efficacy of TMP-301 Compared to Placebo in Adult Patients With Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=110 | Active, not recruiting | Sponsor: Tempero Bio, Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed • Addiction (Opioid and Alcohol)

TMP-301-CUD-102: A Study to Investigate the Interaction Between TMP-301 and Cocaine. (clinicaltrials.gov) - P1 | N=18 | Completed | Sponsor: Tempero Bio, Inc. | Recruiting ➔ Completed | Trial completion date: Aug 2025 ➔ May 2025

Trial completion • Trial completion date

Tempero Bio Secures $70 Million Series B Financing to Advance TMP-301 into Phase 2 Trials for Substance Use Disorders (Tempero Bio Press Release) - "Tempero Bio, Inc...today announced the closing of a $70 million Series B financing. The financing was led by 8VC with participation from Aditum Bio, Khosla Ventures, and other investors. The proceeds will be used to advance TMP-301 through two Phase 2 clinical trials for alcohol use disorder and cocaine use disorder, as well as Phase 3-enabling activities and preclinical studies for additional indications and formulations."

Financing • Addiction (Opioid and Alcohol)

Nxera Pharma’s Partner Tempero Bio Initiates Phase 2 Trial with TMP-301 for Alcohol Use Disorder (GlobeNewswire) - "Nxera Pharma Co., Ltd...announces that its partner Tempero Bio, Inc. has initiated a Phase 2 trial of TMP-301, a potent, selective and orally available mGluR5 negative allosteric modulator (NAM), for the treatment of alcohol use disorder...The Phase 2 study initiated will assess the safety, tolerability and effect on alcohol use of TMP-301 compared to placebo in patients with alcohol use disorder."

Trial status • Addiction (Opioid and Alcohol)

TMP-301-CUD-102: A Study to Investigate the Interaction Between TMP-301 and Cocaine. (clinicaltrials.gov) - P1 | N=18 | Recruiting | Sponsor: Tempero Bio, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open

TMP-301-AUD-201: A Study to Investigate the Safety and Efficacy of TMP-301 Compared to Placebo in Adult Patients With Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=100 | Recruiting | Sponsor: Tempero Bio, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Addiction (Opioid and Alcohol)

A Study to Investigate the Safety and Efficacy of TMP-301 Compared to Placebo in Adult Patients With Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=100 | Not yet recruiting | Sponsor: Tempero Bio, Inc.

New P2 trial • Addiction (Opioid and Alcohol)

A Study to Investigate the Safety and Efficacy of TMP-301 Compared to Placebo in Adult Patients With Cocaine Use Disorder (clinicaltrials.gov) - P1 | N=18 | Not yet recruiting | Sponsor: Tempero Bio, Inc.

New P1 trial

Multiple Ascending Dose Study of TMP-301 in Healthy Subjects (clinicaltrials.gov) - P1 | N=30 | Completed | Sponsor: Tempero Bio, Inc. | Active, not recruiting ➔ Completed

Trial completion • Psychiatry • CYP1A2

Multiple Ascending Dose Study of TMP-301 in Healthy Subjects (clinicaltrials.gov) - P1 | N=32 | Active, not recruiting | Sponsor: Tempero Bio, Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed • Psychiatry • CYP1A2

Multiple Ascending Dose Study of TMP-301 in Healthy Subjects (clinicaltrials.gov) - P1 | N=32 | Recruiting | Sponsor: Tempero Bio, Inc. | Active, not recruiting ➔ Recruiting

Enrollment open • Psychiatry

Multiple Ascending Dose Study of TMP-301 in Healthy Subjects (clinicaltrials.gov) - P1 | N=32 | Active, not recruiting | Sponsor: Tempero Bio, Inc.

New P1 trial • Psychiatry

Study to Investigate the Receptor Occupancy of HTL0014242 Using [18F] FPEB in Healthy Male Subjects (clinicaltrials.gov) - P1; N=8; Completed; Sponsor: Heptares Therapeutics Limited; Recruiting ➔ Completed

Clinical • Trial completion

Phase 1, Healthy Subject, Safety, Tolerability and Pharmacokinetic Study of mGlu5 NAM HTL0014242 (clinicaltrials.gov) - P1; N=71; Completed; Sponsor: Heptares Therapeutics Limited; Recruiting ➔ Completed

Clinical • Trial completion

Study to Investigate the Receptor Occupancy of HTL0014242 Using [18F] FPEB in Healthy Male Subjects (clinicaltrials.gov) - P1; N=10; Recruiting; Sponsor: Heptares Therapeutics Limited; Trial completion date: Mar 2021 ➔ Aug 2021; Trial primary completion date: Mar 2021 ➔ Aug 2021

Clinical • Trial completion date • Trial primary completion date

Understanding exposure-receptor occupancy relationships for metabotropic glutamate receptor 5 (mGlu) negative allosteric modulators across a range of pre-clinical and clinical studies. (PubMed, J Pharmacol Exp Ther) - "The aim of this study was to measure the RO of the mGlu NAM, HTL0014242, in rodents and cynomolgus monkey and to compare its plasma, and brain, exposure-RO relationships with those of clinically tested mGlu NAMs dipraglurant, mavoglurant and basimglurant. Significance Statement Despite the long history of mGlu as a therapeutic target and progression of multiple compounds to the clinic, no formal comparison of exposure-receptor occupancy relationships has been conducted. Our data indicate for the first time that a consistent, unified relationship can be observed between exposure and mGlu receptor occupancy when unbound brain concentration and receptor affinity are taken into account across a range of species for a diverse set of mGlu NAMs, including a new drug candidate, HTL0014242."

Journal

Phase 1, Healthy Subject, Safety, Tolerability and Pharmacokinetic Study of mGlu5 NAM HTL0014242 (clinicaltrials.gov) - P1; N=78; Recruiting; Sponsor: Heptares Therapeutics Limited; Trial completion date: May 2020 ➔ May 2021; Trial primary completion date: Apr 2020 ➔ Jan 2021

Clinical • Trial completion date • Trial primary completion date

Study to Investigate the Receptor Occupancy of HTL0014242 Using [18F] FPEB in Healthy Male Subjects (clinicaltrials.gov) - P1; N=10; Recruiting; Sponsor: Heptares Therapeutics Limited; Trial completion date: Nov 2020 ➔ Mar 2021; Trial primary completion date: Nov 2020 ➔ Mar 2021

Clinical • Trial completion date • Trial primary completion date

Structure-based discovery and development of metabotropic glutamate receptor 5 negative allosteric modulators. (PubMed, Adv Pharmacol) - "An alternative approach to drug discovery is to use structural knowledge to enable structure-based drug design (SBDD), which allows the design of molecules in a more rational, rather than empirical, fashion. Here we will describe the process of SBDD in the discovery of the mGlu negative allosteric modulator HTL0014242 and describe how knowledge of receptor structure can also be used to gain insights into the receptor activation mechanisms."

Journal

Study to Investigate the Receptor Occupancy of HTL0014242 Using [18F] FPEB in Healthy Male Subjects (clinicaltrials.gov) - P1; N=10; Recruiting; Sponsor: Heptares Therapeutics Limited

Clinical • New P1 trial

Phase 1, Healthy Subject, Safety, Tolerability and Pharmacokinetic Study of mGlu5 NAM HTL0014242 (clinicaltrials.gov) - P1; N=78; Recruiting; Sponsor: Heptares Therapeutics Limited; N=48 ➔ 78; Trial completion date: Aug 2019 ➔ May 2020; Trial primary completion date: Jul 2019 ➔ Apr 2020

Clinical • Enrollment change • Trial completion date • Trial primary completion date