Evaluating Relative Bioavailability of OC-01 (Varenicline) Nasal Spray as Compared to Orally Administered Varenicline

NCT04072146 | Completed Phase 1 Results FDA Drug

• 1 other identifier: OPP-100
• Study Type: interventional
• Target: 22
• Locations: 1 country
• Sites: 1

Brief Summary

To assess the relative bioavailability of varenicline administered intranasally at its highest intended clinical strength compared to varenicline administered orally at its highest oral tablet strength.

Conditions

Healthy Subjects

Outcome Measures

Primary Outcomes (4)

• AUC0-t

  Area under the curve from predose (time 0), 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post dose.

  Blood samples were taken predose (time 0), 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post dose.

• AUC0-inf

  AUC0-inf taken at predose (time 0), 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post dose.

  Blood samples were taken predose (time 0), 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post dose.

• Cmax

  Cmax taken at predose (time 0), 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post dose.

  Blood samples were taken predose (time 0), 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post dose.

• Tmax

  Tmax taken at predose (time 0), 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post dose.

  Blood samples were taken predose (time 0), 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post dose.

Other Outcomes (1)

• Creatine Shift From Normal at Baseline to Abnormal After 2 Hours Post-treatment

  Baseline to 2 hours post treatment

Study Arms (2)

Varenicline oral tablet 1mg, then OC-01 (varenicline solution) nasal spray 0.12 mg

EXPERIMENTAL

OC-01 0.12 mg was administered intranasally 50 ul into each nostril in a fasted state

Drug: Vaenicline oral tablet 1 mg, then OC-01 (varenicline solution) nasal spray 0.12 mg

OC-01 (varenicline solution) nasal spray 0.12 mg, then Varenicline oral tablet 1 mg

ACTIVE COMPARATOR

Varenicline oral tablet 1mg was administered orally in a fasted stated with 200 ml water

Drug: OC-01 (varenicline solution) nasal spray 0.12 mg then Varenicline oral tablet 1 mg

Interventions

Vaenicline oral tablet 1 mg, then OC-01 (varenicline solution) nasal spray 0.12 mg DRUG

Cross over bioavailability study

Also known as: varenicline

Varenicline oral tablet 1mg, then OC-01 (varenicline solution) nasal spray 0.12 mg

OC-01 (varenicline solution) nasal spray 0.12 mg then Varenicline oral tablet 1 mg DRUG

Cross over bioavailability study

Also known as: varenicline

OC-01 (varenicline solution) nasal spray 0.12 mg, then Varenicline oral tablet 1 mg

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Body mass index between 18.0 and 32.0 kg/m2, inclusive.
• Healthy as determined by a responsible and experienced physician, based on a medical evaluation including medical history, physical examination, ECG and laboratory tests.
• Have provided verbal and written informed consent
• If a female of childbearing potential who is not using an acceptable means of birth control (acceptable methods of contraception include: hormonal - oral, implantable, injectable, or transdermal contraceptives, mechanical - spermicide in conjunction with a barrier such as a diaphragm or condom, IUD, or surgical sterilization of partner), have a negative urine pregnancy test at the Screening Visit.

You may not qualify if:

• Have had nasal or sinus surgery (including history of application of nasal cautery) or significant trauma to these areas.
• Have a vascularized polyp, severely deviated septum, chronic recurrent nosebleeds, or severe nasal airway obstruction as confirmed by intranasal examination at the Screening Visit.
• Any contraindication to varenicline according to the applicable label.
• Have severe renal impairment (estimated creatinine clearance less than 30mL per minute)
• Have current concomitant use of snuff, chewing tobacco, e-cigarettes or cigarettes/cigars during the study
• Have any condition or history that, in the opinion of the investigator, may interfere with study compliance, outcome measures, safety parameters, and/or the general medical condition of the subject
• Be a female who is pregnant, nursing an infant, or planning a pregnancy at the Screening Visit. Be a woman of childbearing potential who is not using an acceptable means of birth control; acceptable methods of contraception include: hormonal - oral, implantable, injectable, or transdermal contraceptives; mechanical - spermicide in conjunction with a barrier such as a diaphragm or condom; IUD; or surgical sterilization of partner.
• Be currently enrolled in an investigational drug or device study or have used an investigational drug or device within 30 days prior to the Screening Visit.

Sponsors & Collaborators

• Oyster Point Pharma, Inc.: lead

Study Sites (1)

United States, Miami Florida

Miami, Florida, 33136, United States

Location

Related Publications (1)

• Nau J, Wyatt DJ, Rollema H, Crean CS. A Phase I, Open-label, Randomized, 2-Way Crossover Study to Evaluate the Relative Bioavailability of Intranasal and Oral Varenicline. Clin Ther. 2021 Sep;43(9):1595-1607. doi: 10.1016/j.clinthera.2021.07.020. Epub 2021 Aug 27.

  PMID: 34456060 DERIVED

MeSH Terms

Interventions

Nasal Sprays; Varenicline

Intervention Hierarchy (Ancestors)

Aerosols; Colloids; Complex Mixtures; Dosage Forms; Pharmaceutical Preparations; Benzazepines; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Quinoxalines

Results Point of Contact

• Title: Jeffrey Nau
• Organization: Oyster Point Pharma, Inc.

jnau@oysterpointrx.com

609-382-9035

Study Officials

• Jeffrey Nau, PhD

  Oyster Point Pharma, Inc.

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 27, 2019
• First Posted: August 28, 2019
• Study Start: August 26, 2019
• Primary Completion: November 15, 2019
• Study Completion: November 15, 2019
• Last Updated: May 23, 2022
• Results First Posted: May 23, 2022

Record last verified: 2022-05

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)