A Study in Healthy Male Volunteers to Investigate the Safety and Tolerability of a Single Dose of Neosaxitoxin Alone and in Combination With Bupivacaine (With and Without Epinephrine) for Brachial Plexus Blockade

Summary

Neosaxitoxin is a new compound that is in clinical development as local anesthetic for surgical anesthesia and postoperative analgesia.

The primary objective of this study is to evaluate the systemic and local safety and tolerability of ascending doses of neosaxitoxin alone and in combination with fixed doses of bupivacaine (with and without epinephrine), following brachial plexus blockade in healthy male subjects.

Secondary objectives:

* Evaluate the pharmacodynamics (PD) of ascending doses of neosaxitoxin, alone and in combination with fixed doses of bupivacaine (with and without epinephrine), following brachial plexus blockade.
* Characterize the pharmacokinetics (PK) of neosaxitoxin and bupivacaine after brachial plexus blockade with neosaxitoxin alone or different drug combinations: neosaxitoxin and epinephrine, neosaxitoxin and bupivacaine, or neosaxitoxin and bupivacaine and epinephrine.

Conditions

• Anesthesia
• Anesthesia, Local
• Analgesia

Interventions

COMBINATION_PRODUCT

Neosaxitoxin combined with bupivacaine low and epinephrine (T1)

A single injection: Neosaxitoxin from 1.25 to 60 µg. Bupivacaine 40 mg. Epinephrine 100 µg.

COMBINATION_PRODUCT

Bupivacaine low combined with epinephrine (C1)

A single injection: Bupivacaine 40 mg. Epinephrine dose 100 µg.

COMBINATION_PRODUCT

Bupivacaine high combined with epinephrine (C2)

A single injection: Bupivacaine 100 mg. Epinephrine 100 µg.

COMBINATION_PRODUCT

Neosaxitoxin combined with bupivacaine low (T2)

A single injection: Neosaxitoxin from 1.25 to 60 μg. Bupivacaine from 10 to 80 mg.

DRUG

Bupivacaine low (C3)

A single injection: Bupivacaine from 10 to 80 mg.

DRUG

Bupivacaine high (C4)

A single injection: Bupivacaine 100 mg.

DRUG

Neosaxitoxin (T3)

A single injection: Neosaxitoxin will be between 1.25 and 60 µg.

COMBINATION_PRODUCT

Neosaxitoxin combined with epinephrine (T4)

A single injection: Neosaxitoxin will be between 1.25 and 60 μg. Epinephrine 100 µg.

COMBINATION_PRODUCT

Neosaxitoxin combined with bupivacaine low and epinephrine

A single injection: Neosaxitoxin will be between 1.25 to 60 µg. Bupivacaine dose based on results from Part B (10 to 80 mg). Epinephrine 100 µg.

COMBINATION_PRODUCT

Neosaxitoxin combined with bupivacaine low

A single injection: Neosaxitoxin will be between 1.25 to 60 μg. Bupivacaine dose based on results from Part B (10 to 80 mg).

Sponsors & Collaborators

• Grünenthal GmbH

  lead INDUSTRY

Principal Investigators

• Study Director · Grünenthal GmbH

Study Design

Allocation

RANDOMIZED

Purpose

OTHER

Masking

TRIPLE

Model

PARALLEL

Eligibility

Min Age

18 Years

Max Age

55 Years

Sex

MALE

Healthy Volunteers

Yes

Timeline & Regulatory

Start

2018-01-30

Primary Completion

2018-09-21

Completion

2018-09-21

Countries

• Netherlands

Study Locations