THC-valine-hemisuccinate (SBI-100) / Skye Biosci - LARVOL DELTA

Phase 1 safety, tolerability and pharmacokinetic study of topical ocular CB1 agonist, SBI-100 a novel prodrug of THC, in healthy volunteers (ARVO 2024) - "SBI-100 OE was generally well tolerated. No apparent systemic side effects that could be attributed to systemic exposure to THC were observed. The most reported TEAE was instillation site pain, but this generally resolved within 15 minutes and was not associated with hyperaemia."

Clinical • P1 data • PK/PD data • Glaucoma • Ophthalmology

A study to evaluate the Safety, Tolerability, and Pharmacokinetics of SBI-100 Ophthalmic Emulsion in Healthy Adult Participants (ANZCTR) - P1 | N=48 | Completed | Sponsor: Skye Biosciences,Inc. | Recruiting ➔ Completed

Trial completion • Glaucoma • Ophthalmology

Phase 2, Placebo-Controlled, Study Assessing the Safety and Ocular Efficacy of SBI-100 Ophthalmic Emulsion in Patients With Elevated Eye Pressure (clinicaltrials.gov) - P2 | N=56 | Completed | Sponsor: Skye Bioscience, Inc. | Recruiting ➔ Completed | Trial completion date: Oct 2024 ➔ Feb 2024

Trial completion • Trial completion date • Cardiovascular • Glaucoma • Ophthalmology

Phase 2, Placebo-Controlled, Study Assessing the Safety and Ocular Efficacy of SBI-100 Ophthalmic Emulsion in Patients With Elevated Eye Pressure (clinicaltrials.gov) - P2 | N=54 | Recruiting | Sponsor: Skye Bioscience, Inc.

Trial completion date • Trial primary completion date • Cardiovascular • Glaucoma • Ophthalmology

Phase 2, Placebo-Controlled, Study Assessing the Safety and Ocular Efficacy of SBI-100 Ophthalmic Emulsion in Patients With Elevated Eye Pressure (clinicaltrials.gov) - P2 | N=54 | Recruiting | Sponsor: Skye Bioscience, Inc.

New P2 trial • Cardiovascular • Glaucoma • Ophthalmology

Impact of mucoadhesive agent inclusion on the intraocular pressure lowering profile of Δ-tetrahydrocannabinol-valine-hemisuccinate loaded nanoemulsions in New Zealand white rabbits. (PubMed, Int J Pharm) - "A comparative evaluation of the IOP lowering activity of THC-VHS-NEC, THC-VHS-NE, THC-NEC, and commercial latanoprost ophthalmic solution, was undertaken in normotensive New Zealand white rabbits. A change in formulation pH, surfactant concentration, or sterilization process did not impact the IOP lowering activity of THC-VHS-NEC. Overall, inclusion of a mucoadhesive agent in THC-VHS-NE formulation, significantly increased the duration of activity, and could lead to a once- or twice- a day dosing regimen."

Journal • Preclinical • Ophthalmology

"$SKYE Skye Bioscience Completes THCVHS IND-enabling In Vitro Genotoxicity Studies https://t.co/u0IoGX7pTJ" (@otcdynamics)

Preclinical

Emerald Bioscience Launches Rebrand Including Name Change to Skye Bioscience (Streetinsider.com) - "Skye Bioscience, Inc....has changed its name from Emerald Bioscience, Inc. to Skye Bioscience, Inc. The Company will trade under its new ticker symbol, 'SKYE,' on the OTC effective at market open on Tuesday, January 19, 2021....Since September, our Company has made significant progress on its development plan for its lead molecule, THCVHS...we plan to conduct additional important preclinical studies to further validate intraocular-pressure-lowering activity as well as the potential neuroprotective benefits of our drug....Our first clinical trial planned to start in the third quarter of this year and provide data readouts in Q2 2022."

Clinical data • Commercial • New trial • Preclinical • Glaucoma • Ophthalmology

Effect of surfactant concentration and sterilization process on intraocular pressure-lowering activity of Δ-tetrahydrocannabinol-valine-hemisuccinate (NB1111) nanoemulsions. (PubMed, Drug Deliv Transl Res) - "The IOP lowering effect of the lead formulations, commercial timolol, and latanoprost ophthalmic solutions, as well as an emulsion in Tocrisolve™ (THC-VHS-TOC), was studied in New Zealand White rabbits following topical administration. The formulation could be sterilized by filtration without impacting product attributes. Overall, the optimized THC-VHS-NE formulation demonstrated a significantly better IOP reduction profile in the test model compared to the commercial ophthalmic solutions evaluated."

Journal • Glaucoma • Ophthalmology

Emerald Bioscience Provides Update on Recent Progress and Expected 2020 Milestones (GlobeNewswire, Emerald Bioscience, Inc.) - "Company prepares to enter the clinic in 2020 to test NB1111 (THCVHS) in glaucoma . First patents have been issued for CBDVHS in pursuit of a global patent footprint to complement the IP estate for THCVHS...The Company opened an Australian affiliate in advance of conducting a Phase 1 and Phase 2a study in Australia, among healthy volunteers and patients with glaucoma or ocular hypertension; the studies are planned to be initiated in the second half of 2020 with outcomes data expected at the end of 2020 and early 2021."

New P1 trial • New P2a trial • P1 data • P2a data

IOP-Lowering Ability of NB-1111 Active Moiety, THC, in a Human Tissue Model (AAO 2019) - "Outflow increased from 0.35 ± 0.07 to 0.85 ± 0.21 mL/min/mm2/mmHg for normotensive and 0.26 ± 0.10 to 0.74 ± 0.16 mL/min/mm2/mmHg for glaucomatous samples (N ≥12; P < .05 and P < .001; respectively). Conclusion The ability of THC to lower IOP may be due to an antifibrotic mechanism in addition to a known vasodilatory effect."

Emerald Bioscience to present research data related to its glaucoma drug candidate, NB1111, at 2019 American Association of Pharmaceutical Scientists (GlobeNewswire) - "Emerald Bioscience...will present preclinical data evaluating the superiority of its prodrug of tetrahydrocannabinol (THC), NB1111, in lowering intraocular pressure in a multi-dose normotensive rabbit model when compared to the current standards of care in glaucoma treatment, timolol and latanoprost, at the 2019 American Association of Pharmaceutical Scientists Meeting (AAPS) being held November 3 -6, 2019, at the Henry B. Gonzalez Convention Center in San Antonio, Texas."

PK/PD data • Preclinical

"Using 3D tissue #model of hypertensive #glaucoma, #Glauconix validates MoA of @Emerald_Bio’s NB1111 #AAO2019 hears #THC #prodrug ↓ intraocular pressure & ↓ #biomarkers of #inflammation & #fibrosis https://t.co/3K0L1vKVB0 #cannabinoids #ophthalmology @aao_ophth" (@DDNewsOnline)

Biomarker

IOP Profiles Following Single-Dose ?9-Tetrahydrocannabinol-Valine-Hemisuccinate (NB1111) Nanoemulsion and Latanoprost (AAO 2019) - "There were no signs of irritation observed from any of the formulations. Conclusion Overall, THC-VHS NEC demonstrates a superior IOP-lowering profile (P < .05) compared to the marketed LAT ophthalmic solution."

Glauconix Presents Data Validating Impact of Emerald Bioscience’s Prodrug on the Ocular Endocannabinoid System in Glaucoma (GlobeNewswire, Emerald Bioscience, Inc.) - "Emerald Bioscience, Inc...announced data validating mechanisms of action of its drug candidate, NB1111...by testing the active component of the prodrug, THC, in human donor tissue...Emerald anticipates performing two human clinical trials in 2020, both in Australia, examining the effects of NB1111 on normal eyes as well as among patients with either glaucoma or underlying ocular hypertension..."

Clinical • New trial

Emerald Bioscience’s NB1111 Demonstrates Superiority in Lowering Intraocular Pressure Compared to Global Standard of Care Glaucoma Treatment in Preclinical Model (GlobeNewswire, Emerald Bioscience, Inc.) - "Emerald Bioscience, Inc...announced data demonstrating the superiority of its advanced formulation of NB1111...in lowering intraocular pressure (IOP) in the eye in a validated animal model...The data was presented at the 2019 American Academy of Ophthalmology Annual Meeting (AAO)...'These are important experiments prior to initiating multiple human studies, which we project will be conducted throughout 2020.'"

New trial • Preclinical

IOP-Lowering Ability of NB-1111 Active Moiety, THC, in a Human Tissue Model (AAO 2019) - No abstract available.

Glauconix Biosciences and University of Mississippi to present research data related to Emerald Bioscience’s glaucoma drug candidate, NB1111, at 2019 American Academy of Ophthalmology Annual Meeting (GlobeNewswire) - "...Glauconix Biosciences, Inc. will be presenting biomarker data in human donor tissue related to the mechanism of action of...NB1111, a prodrug of tetrahydrocannabinol (THC-valine-hemisuccinate; THCVHS), at the 2019 American Academy of Ophthalmology Annual Meeting (AAO) being held October 12 -15, 2019, at the Moscone Center in San Francisco, CA...Additionally, the company will be featured in a poster session showcasing NB1111 superiority in lowering intraocular pressure (IOP) in a validated animal model..."

Biomarker • Preclinical

Emerald Bioscience starts Australian operation ahead of planned glaucoma study (GlobeNewswire) - "Emerald Bioscience, Inc....announced today that the company has opened its Australian office. The formation of EMBI Australia Pty Ltd and opening of an Australian office is an important step in meeting regulatory requirements to conduct studies in Australia and represents EMBI’s commitment to initiate its first-in-human study of NB1111...in the indication of glaucoma...The Australian office will serve as a key gateway for our future clinical studies with NB1111...."

Clinical