funapide extended release (PCRX301) / Xenon, Pacira - LARVOL DELTA

Conservation of triplet-triplet energy transfer photoprotective pathways in fucoxanthin chlorophyll-binding proteins across algal lineages. (PubMed, Biochim Biophys Acta Bioenerg) - "Furthermore, despite the marked change in the pigment content of E-FCP with growth light intensity, the TTET pathway is not affected. Thus, our comparative investigation of FCPs revealed a photoprotective TTET pathway shared within these classes involving the fucoxanthin in site Fx301, a site exposed to the exterior of the antenna monomer that has no equivalent in Light-Harvesting Complexes from the green lineage."

Journal

Study to Evaluate the Safety and Tolerability of FX301 in Patients Undergoing Bunionectomy (clinicaltrials.gov) - P1 | N=85 | Completed | Sponsor: Flexion Therapeutics, Inc. | Active, not recruiting ➔ Completed

Trial completion • Pain

Study to Evaluate the Safety and Tolerability of FX301 in Patients Undergoing Bunionectomy (clinicaltrials.gov) - P1 | N=85 | Active, not recruiting | Sponsor: Flexion Therapeutics, Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed • Pain

Study to Evaluate the Safety and Tolerability of FX301 in Patients Undergoing Bunionectomy (clinicaltrials.gov) - P1; N=84; Recruiting; Sponsor: Flexion Therapeutics, Inc.; Trial completion date: Oct 2021 ➔ Mar 2022

Clinical • Trial completion date • Pain

Study to Evaluate the Safety and Tolerability of FX301 in Patients Undergoing Bunionectomy (clinicaltrials.gov) - P1; N=84; Recruiting; Sponsor: Flexion Therapeutics, Inc.

New P1 trial • Pain

Flexion Therapeutics Announces FDA Clearance of Investigational New Drug Application for FX301, a Novel Formulation of a Locally Administered NaV1.7 Inhibitor for Post-Operative Pain (GlobeNewswire) - "Flexion Therapeutics...today announced the U.S. Food and Drug Administration (FDA) cleared the Investigational New Drug (IND) application for FX301....The FDA’s clearance of the IND was supported by key preclinical data...Flexion plans to initiate a Phase 1b proof of concept clinical trial of FX301 administered as a popliteal fossa block (a commonly used nerve block in foot and ankle-related surgeries) in patients undergoing bunionectomy and expects to treat the first patient in the first half of this year. Topline results from the trial are anticipated in late 2021."

IND • New P1 trial • P1 data • CNS Disorders • Pain

"$FLXN Flexion Therapeutics Announces FDA Clearance of Investigational New Drug Application for FX301, a Novel Formulation of a Locally Administered NaV1.7 Inhibitor for Post-Operative Pain https://t.co/6u3a6SjBMP" (@stock_titan)

FDA event • IND • Pain

Xenon Pharmaceuticals Reports Third Quarter 2020 Financial Results and Provides Corporate Update (Xenon Pharmaceuticals Press Release) - "The initial development of FX301 is intended to support administration as a peripheral nerve block for control of post-operative pain. Flexion anticipates filing an IND application in the first half of 2021 to support a proof-of-concept clinical trial of popliteal fossa block with FX301 in patients undergoing bunionectomy. Results from that trial could potentially be available in late 2021."

Clinical data • IND • CNS Disorders • Pain

[VIRTUAL] Selective Pharmacology Of A Na V 1.7 Antagonist Hydrogel In A Pig Model Of Nerve Block (ASA 2020) - "The effects of FX301 on sensory and motor function following sciatic nerve block were assessed in a validated pain model in pigs, and the pharmacokinetics of funapide release from the hydrogel formulation were measured in plasma and local tissue following injection. 18 young adult pigs were anesthetized, 10 mL of vehicle, FX301 (13 mg/mL), or liposomal bupivacaine (LB) (13.3 mg/mL) was injected via ultrasound-guidance close to the sciatic nerve, and a 5cm surgical incision was created in the ipsilateral hind leg. Prior to the procedure and at 1, 4, 8, 12, 24, 36, 48, and 72h post-procedure, analgesic effect was evaluated by von Frey testing and General Behavior Scoring (GBS), and plasma samples were collected... von Frey testing showed an increase in withdrawal force following FX301 treatment. (Figure 1A ) Withdrawal force (vs vehicle) was significantly higher in pigs treated with FX301 at 36h, but only through 8h with LB. GBS scores were highest in vehicle, indicating..."

Anesthesia • Pain

Flexion Therapeutics Announces Podium Presentation of FX301 Preclinical Data at Virtual ANESTHESIOLOGY 2020 Meeting (GlobeNewswire) - "Flexion Therapeutics, Inc....today announced the podium presentation of preclinical efficacy and pharmacokinetic (PK) data for FX301, its locally administered peripheral nerve block candidate for control of post-operative pain at the virtual ANESTHESIOLOGY 2020 meeting....Flexion remains on track to file the Investigational New Drug (IND) application and initiate clinical trials in 2021."

IND • New trial • Preclinical • CNS Disorders • Pain

Flexion Therapeutics Reports Second-Quarter 2020 Financial Results and Recent Business Highlights (GlobeNewswire) - "Net sales of ZILRETTA were $15.5 million and $17.0 million for the three months ended June 30, 2020 and 2019, respectively....In total, approximately 36,700 units of ZILRETTA were purchased in the second quarter, which is essentially in line with the first quarter of 2020....Also in May, Flexion restarted enrollment in the Phase 1...of FX201, its investigation gene therapy product candidate for OA....The Company anticipates initiating FX301 clinical trials in 2021. In addition, the Company intends to initiate a trial investigating ZILRETTA in shoulder OA in 2021....Flexion announced plans to recommence manufacturing in the fourth quarter of this year to help ensure adequate and uninterrupted supply of ZILRETTA to meet future demand."

Commercial • New trial • Sales • Trial status • Osteoarthritis • Pain

Flexion Therapeutics reports first-quarter 2020 financial results and recent business highlights (GlobeNewswire) - "Effectively all medical and scientific congresses scheduled for the spring of 2020 have been cancelled due to the COVID-19 pandemic. As a result, the following abstracts and posters have been published online:...Osteoarthritis Research International (OARSI)/Osteoarthritis & Cartilage: Prospective Radiographic Analysis of the Effect of Single and Repeat Administrations of Intra-Articular Corticosteroids in Knee Osteoarthritis (Abstract 741); Fitbit®-Derived Evidence of Enhanced Mobility of Patients with Knee OA Treated with ZILRETTA: Results from a Phase 3b, Single-Arm, Open-Label (Abstract 745); A Thousand Patient Voices: Knowledge, Impact, and Experiences of Living with OA of the Knee (Abstract 735); American Society of Regional Anesthesia and Acute Pain Medicine: Efficacy and PK of Peripheral Nerve Block by FX301, a Novel Nav1.7 Antagonist Hydrogel, in a Postoperative Pain Model in Pigs (Poster 1169)"

Clinical data • P3 data • Preclinical • CNS Disorders • Infectious Disease • Inflammation • Orthopedics • Osteoarthritis • Pain

Flexion Therapeutics Announces Positive Preclinical Data Supporting Development of FX301, a Locally Administered Nav1.7 Inhibitor Product Candidate for Post-Operative Pain (GlobeNewswire, Flexion Therapeutics, Inc.) - "New animal data show FX301 provided sustained, post-operative analgesic effect with no impairment in motor function compared to liposomal bupivacaine and placebo . High local concentrations of funapide, the active ingredient in FX301, were measured at the site of administration for the duration of the study, consistent with the creation of a depot providing controlled drug release. 'In contrast to liposomal bupivacaine, FX301, through its innovative mechanism of action, provided improved analgesic effect while preserving motor function...We look forward to advancing the FX301 GLP toxicology studies this year and intend to initiate human trials in 2021.'"

New trial • Preclinical • Anesthesia • CNS Disorders • Pain

Flexion Therapeutics announces Zilretta license agreement and provides business update amid coronavirus pandemic (GlobeNewswire) - "Temporary Suspension of Clinical Trials: Flexion is temporarily suspending its active clinical trials including the Phase 1 trial evaluating the safety and tolerability of FX201...in patients with osteoarthritis (OA) of the knee, and the Phase 2 trial evaluating the efficacy of ZILRETTA in patients with shoulder OA or adhesive capsulitis....The company continues to advance the preclinical program for FX301, its product candidate being developed as a locally administered peripheral nerve block for control of post-operative pain. Flexion continues to anticipate the initiation of FX301 clinical trials in 2021."

Trial initiation date • Trial status • Trial suspension

Flexion Therapeutics reports fourth-quarter and full-year 2019 financial results (GlobeNewswire) - "In September, Flexion entered into a definitive agreement with Xenon Pharmaceuticals that provides the Company with the global rights to develop and commercialize XEN402, a NaV1.7 inhibitor, known as funapide, for control of post-operative pain. The new preclinical product candidate, known as FX301, consists of XEN402 formulated for extended release from a thermosensitive hydrogel for administration as a peripheral nerve block for control of post-operative pain. Flexion held a pre-IND meeting with FDA in January and remains on track to initiate FX301 clinical trials in 2021."

IND • Licensing / partnership • New trial