Phase I Pharmacokinetic Study of RX0041-2

Systemic Pharmacokinetics of Acute, Topical, Intranasal Administration of RX0041-002 in Healthy Male and Female Subjects

This Phase I study is to examine the systemic pharmacokinetics of RX0041-002 following acute, topical, intranasal administration to healthy male and female volunteers.

Study Overview

• Status: Completed
• Conditions: Drug Reaction to Analgesic Nos
• Intervention / Treatment: Drug: RX0041-2

Detailed Description

This is a Phase I, single dose, single-center, open-label study of the plasma and urinary pharmacokinetics of RX004-002 and its major metabolites in male and female healthy subjects.

• Study Type: Interventional
• Enrollment (Actual): 30
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years and older (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

1. Male or female ≥18 but ≤ 80 years of age at the time of dosing.
2. BMI ≥ 18 and ≤ 32 at the screening visit.
3. Females (if of child-bearing potential and sexually active) and males (if sexually active with a partner of child-bearing potential) who agree to use a medically acceptable and effective birth control method from the first dose and for 8 days following administration of study drug. Medically acceptable methods of contraception that may be used by the participant and/or his/her partner include abstinence, birth control pills or patches, diaphragm, intrauterine device (IUD), condom, surgical sterilization, and progestin implant or injection. Prohibited methods include: the rhythm method or withdrawal.
4. Willing and able to provide written informed consent and able to understand and comply with protocol requirements.
5. During the period of study confinement, subjects will be required to abstain from beverages containing grapefruit juice or caffeine.

Exclusion Criteria:

1. Has a known allergy to any ester based anesthetics including cocaine HCl, procaine, tetracaine, chloroprocaine, dibucaine, or benzocaine Amide based anesthetic allergies are NOT exclusionary. Amide based anesthetics are: Lidocaine, mepivicaine, bupivicaine, levobupivicaine, ropivicaine, etidocaine, prilocaine, and articaine.
2. The use of amphetamines, methylphenidate or other stimulant prescription and nonprescription products such as pseudoephedrine, bronchial inhalers containing sympathomimetics (epinephrine or other beta-receptor agonist) or herbal products in the 7 days prior to screening or has a need to use these drugs during the course of the study.
3. Use of any SNRIs/SSRIs antidepressants or tricyclic antidepressant up to7 days or 5 half-lives (whichever is longer) prior to screening or has a need to use these drugs during the screening period and throughout the time period of the trial.
4. Use of MAO Inhibitor drugs up to14 days prior to screening or has a need to use these drugs during the screening period and throughout the time period of the trial.
5. Has a history of abuse of controlled substances, nasal or otherwise, or has damage to the nasal space, that in the opinion of the investigator might interfere with the ability to absorb RX0041-002.
6. Has severely traumatized mucosa or sepsis in the nasal cavity.
7. Has participated in an investigational study or received an investigational drug within 30 days preceding the randomization.
8. Is a pregnant or nursing mother.
9. Has a positive pregnancy test at Screening or Day 1.
10. Has a history of seizure, with the exception of febrile seizures.
11. Has glaucoma, symptomatic cardiovascular disease, or moderate to severe hypertension (defined as an average SBP ≥160 mmHg or an average DBP ≥ 100 mmHg at the dosing visit).
12. Has a known personal or family history of hereditary pseudocholinesterase deficiency. Study participants will be screened by asking about personal or family history of anesthetic reaction, anesthetic death, and previous diagnosis of psuedocholinesterase deficiency in a relative or personally. Subjects identified with pseudocholinesterase deficiency are at risk for delayed recovery with certain anesthetics (e.g. succinylcholine and ester-based anesthetics).
13. Has a known personal or family history of pheochromocytoma. Study participants will be specifically asked if they have been treated for a pheochromocytoma previously or if they have a family member who has been diagnosed with pheochromocytoma (since 10% of these are familial).
14. Has a known personal or family history of adrenal tumor.
15. ECG abnormalities judged clinically significant by the investigator.
16. Has a positive urine test result for drugs of abuse (amphetamines, barbiturates, cannabinoids, cocaine metabolites, opiates and oxycodone) at Screening or Day 1
17. Hematocrit, WBC, or platelets outside the normal limits and judged clinically significant by the investigator.
18. Serum potassium outside normal limits and judged clinically significant by the investigator.
19. Serum ALT, AST, and bilirubin exceeding 2X ULN for the lab's reference values.
20. Evidence of impaired renal function based upon laboratory tests and investigator opinion.
21. Clinical chemistry abnormalities judged clinically significant by the investigator.
22. Donation of blood (one pint or greater) within four weeks prior to administration of study medication.
23. Not suitable for entry into the study in the opinion of the investigator.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Single-dose, open label RX0041-2; Active Drug	Drug: RX0041-2; Pharmacokinetic study; Other Names: TS

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetic Measurement of RX0041	Cmax of RX0041	24 Hours
Pharmacokinetic Measurement of RX0041	AUC of RX0041	24 Hours

Collaborators and Investigators

• Sponsor: Pharmaceutical Project Solutions, Inc.
• Investigators: Study Director: Melissa L Goodhead, MSc, Clinical/Regulatory Agent

Study record dates

Study Major Dates

• Study Start: October 1, 2015
• Primary Completion (Actual): October 1, 2015
• Study Completion (Actual): October 1, 2015

Study Registration Dates

• First Submitted: January 18, 2016
• First Submitted That Met QC Criteria: January 25, 2016
• First Posted (Estimate): January 28, 2016

Study Record Updates

• Last Update Posted (Estimate): January 28, 2016
• Last Update Submitted That Met QC Criteria: January 25, 2016
• Last Verified: January 1, 2016

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Chemically-Induced Disorders; Drug-Related Side Effects and Adverse Reactions
• Other Study ID Numbers: 2015016

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: Undecided