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CompletedNCT01304316Updated Aug 31, 2017Results posted

Dose-Escalation Safety and Pharmacokinetic Study of K305

A Phase 2 interventional study of Tetracaine HCl 3% and Oxymetazoline HCl 0.05% in Anesthesia, sponsored by St. Renatus, LLC. Completed at 1 site in United States. Open to participants aged 18 Years and older, including healthy volunteers. Per ClinicalTrials.gov, last updated 2017-08-31.

Sponsored by St. Renatus, LLC · Phase 2, Interventional, and Supportive care

Phase
Phase 2
Study type
Interventional
Enrollment
12
Allocation
Not applicable
Ages
18 Years and older
Sex
All
01

Study summary

The purpose of this study is to determine the pharmacokinetics/pharmacodynamics and safety of a nasal spray containing the anesthetic drug tetracaine in combination with oxymetazoline

Read the detailed description

The purpose of this study was to determine the safety and pharmacokinetics of the standard dose of intranasal Kovacaine Mist of 0.6 mL (18 mg tetracaine HCl with 0.3 mg oxymetazoline HCl) and a proposed maximum recommended dental dose of 1.2 mL (36 mg tetracaine HCl with 0.6 mg oxymetazoline HCl). The primary objectives were to determine if either dose significantly changed blood pressure readings (systolic and diastolic), pulse rate, or oxygen saturation levels from baseline pretreatment values and to determine the safety profile of both doses. The secondary objectives were to establish the pharmacokinetics of oxymetazoline, tetracaine, and its major metabolite (parabutylaminobenzoic acid) following the intranasal administration of both doses. Each subject received the standard dose (3 sprays in each nostril with 4 minutes between each pair of sprays) followed 1 to 3 weeks later by the high dose (as 6 sprays in each nostril).

02

Conditions studied

  • Anesthesia
03

In context

Lead sponsor

St. Renatus, LLC is the lead sponsor of 11 studies on the registry; none are open to participants now.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years and older
Sexes eligible
All
Accepts healthy volunteers
Yes

Inclusion criteria

  • Male or female between 18 and 65 years of age
  • BMI between19 and 29 kg/m2
  • Sufficiently healthy as determined by the investigator to receive the test medications and undergo the scheduled study procedure
  • Can breathe through both nostrils
  • Females of child-bearing potential must have a negative urine pregnancy test and must have been using adequate means of birth control for at least one month prior to study entry and during the study
  • Screening BP ≤ 140/90
  • Screening SpO2 ≥ 96
  • Can understand and sign the informed consent document
  • Can communicate with the investigator
  • Can understand and comply with the requirements of the protocol.

Exclusion criteria

Exclusion Criteria:

  • A clinically relevant history or presence of respiratory, thyroid, gastrointestinal, renal, hepatic, hematological, lymphatic, cardiovascular, psychiatric, neurologic, musculoskeletal, genitourinary, infective, inflammatory, immunological, dermatological, or connective tissue disease or disorder or a clinically relevant history or presence of narrow angle glaucoma and in men benign prostatic hypertrophy, Hashimoto"s Thyroiditis, lymphocytic thyroiditis, or uncontrolled diabetes
  • Clinically significant abnormalities in laboratory values
  • Clinically relevant sinus/nasal surgical history
  • Current condition, such as nasal congestion or sinus infection, that may influence responses to study medication
  • History of recurrent nose bleeds
  • History of pseudocholinesterase deficiency or previous prolonged paralysis with succinylcholine or "difficulty waking up from general anesthesia"
  • Allergic to or intolerant of tetracaine, benzocaine, other ester local anesthetics, or para-aminobenzoic acid (as found in PABA-containing sunscreens)
  • Allergic to or intolerant of oxymetazoline or preservatives found in these solutions
  • History of alcoholism and/or drug abuse
  • Have taken a monamine oxidase inhibitor, or vasopressor drug within the past 3 weeks
  • Have received or taken local anesthetics within 72 hours of the first or second treatment visits
  • Are nursing, pregnant, suspected of being pregnant, or trying to become pregnant (Females will be required to take a urine pregnancy test at each study visit to rule out pregnancy)
  • Have used any investigational drug and/or participated in any clinical trial within 30 days of baseline
05

Study design

Phase
Phase 2
Primary purpose
Supportive care
Allocation
Not applicable
Intervention model
Single group
Masking
None (open label)
Enrollment
12 participants (actual)

Study arms

  • Experimental
    Kovacaine Nasal Spray

    Tetracaine HCl 3% and Oxymetazoline HCl 0.05%: 6 sprays of 0.1 mL - total of 18 mg tetracaine HCl and 0.3 mg oxymetazoline HCl followed by 12 sprays of 0.1 mL - total of 36 mg tetracaine HCl and 0.6 mg oxymetazoline HCl

    Drug: Tetracaine HCl 3% and Oxymetazoline HCl 0.05%

Interventions

  • DrugTetracaine HCl 3% and Oxymetazoline HCl 0.05%

    Tetracaine HCl 3% and Oxymetazoline HCl 0.05%

    Also known as: Kovacaine Nasal Spray

06

What researchers measure

Primary outcomes

  1. Cmax of Oxymetazoline

    Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

  2. Cmax of Tetracaine

    Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

  3. Cmax of PBBA

    Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

  4. Half Life of Oxymetazoline

    Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

  5. Half Life of Tetracaine

    Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

  6. Half Life of PBBA

    Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

Secondary outcomes

  1. Pulse Oximetry Maximum Change From Baseline

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

  2. Diastolic BP Maximum Change From Baseline

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

  3. Systolic BP Maximum Change From Baseline

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

  4. Pulse Rate Maximum Change From Baseline

    Time frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

07

Results

Posted Aug 31, 2017

Participant flow

Participant flow — Overall Study
MilestoneKovacaine Nasal Spray
Started12
Completed12
Not completed0

Outcome measures

PrimaryCmax of Oxymetazoline

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · ng/mL
Cmax of Oxymetazoline
ng/mLKovacaine Nasal Spray
0.3 mg1.45 ± 0.473
0.6 mg2.05 ± 0.748
PrimaryCmax of Tetracaine

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · ng/mL
Cmax of Tetracaine
ng/mLKovacaine Nasal Spray
18 mg0.243 ± 0.113
36 mg1.15 ± 2.45
PrimaryCmax of PBBA

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · ng/mL
Cmax of PBBA
ng/mLKovacaine Nasal Spray
Standard Dose492 ± 189
High Dose886 ± 289
PrimaryHalf Life of Oxymetazoline

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · h
Half Life of Oxymetazoline
hKovacaine Nasal Spray
0.3 mg2.32 ± 0.86
0.6 mg1.72 ± 0.46
PrimaryHalf Life of Tetracaine

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes

No measurements were reported for this outcome.

PrimaryHalf Life of PBBA

Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group

Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · h
Half Life of PBBA
hKovacaine Nasal Spray
Standard dose1.00 ± 0.33
High dose1.01 ± 0.32
SecondaryPulse Oximetry Maximum Change From Baseline
Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · % oxygen
Pulse Oximetry Maximum Change From Baseline
% oxygenKovacaine Nasal Spray
Standard K305 Dose0.9 ± 0.9
High K305 Dose0.3 ± 0.65
SecondaryDiastolic BP Maximum Change From Baseline
Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · mmHg
Diastolic BP Maximum Change From Baseline
mmHgKovacaine Nasal Spray
Standard K305 Dose10.8 ± 7.74
High K305 Dose11.7 ± 8.28
SecondarySystolic BP Maximum Change From Baseline
Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · mmHg
Systolic BP Maximum Change From Baseline
mmHgKovacaine Nasal Spray
Standard K305 Dose10.7 ± 7.67
High K305 Dose14.7 ± 8.60
SecondaryPulse Rate Maximum Change From Baseline
Time frame:
Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes
Reported as:
Mean · bpm
Pulse Rate Maximum Change From Baseline
bpmKovacaine Nasal Spray
Standard K305 Dose5.2 ± 4.39
High K305 Dose8.5 ± 8.25

Adverse events

Collected over 2 to 3 weeks. Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Standard K305 Dose—0/12 (0%)8/12 (66.7%)
High K305 Dose—0/12 (0%)12/12 (100%)
Most frequent other events
Showing 10 of 17
Most frequent other events
EventStandard K305 DoseHigh K305 Dose
Nasal congestionRespiratory, thoracic and mediastinal disorders5/129/12
RhinorrhoeaRespiratory, thoracic and mediastinal disorders6/129/12
Nasal discomfortRespiratory, thoracic and mediastinal disorders0/124/12
HeadacheNervous system disorders3/123/12
EpistaxisRespiratory, thoracic and mediastinal disorders2/121/12
Throat irritationRespiratory, thoracic and mediastinal disorders0/122/12
Upper-airway cough syndromeRespiratory, thoracic and mediastinal disorders0/122/12
TinnitusEar and labyrinth disorders0/121/12
NauseaGastrointestinal disorders0/121/12
VomitingGastrointestinal disorders0/121/12

Baseline characteristics

Age, Continuous
Age, Continuous(years)Kovacaine Nasal Spray
Mean30.2 ± 7.45
Sex: Female, Male
Sex: Female, Male(Participants)Kovacaine Nasal Spray
Female6
Male6
Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)Kovacaine Nasal Spray
Hispanic or Latino1
Not Hispanic or Latino11
Unknown or Not Reported0
Race (NIH/OMB)
Race (NIH/OMB)(Participants)Kovacaine Nasal Spray
American Indian or Alaska Native0
Asian1
Native Hawaiian or Other Pacific Islander0
Black or African American1
White10
More than one race0
Unknown or Not Reported0
08

Study locations

1 site
  • University of Pennsylvania, School of Dental Medicine
    Philadelphia, Pennsylvania 19104, United States
09

References and documents

Individual participant data

Plan to share: Undecided

No publications or documents are linked to this record.

10

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Aug 31, 2017, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
11

Registry details

Key details

Study ID
NCT01304316
Lead sponsor
St. Renatus, LLC
Collaborators
Ground Zero Pharmaceuticals, Rho, Inc.
Responsible party
Sponsor
First posted
Feb 25, 2011
Start date
Sep 2010
Primary completion
Nov 2010
Completion
Nov 2010
Results posted
Aug 31, 2017
Last update
Aug 31, 2017

Study contacts

Elliot V Hersh, DMD, MS, PhD
principal investigator · University of Pennsylvania

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

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This study is completed, as verified in Jul 2017. You cannot join it, but the record below documents what was studied.

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