Clinical trial NCT01318226 (phase 2, status: completed)
Conditions: postherpetic neuralgia
ICD codes: B02.22
Drugs: atx08-001, placebo
SMILES: CN1C(=O)C=C(N2CCC[C@@H](N)C2)N(CC2=C(C=CC=C2)C#N)C1=O
Eligibility criteria:

        Inclusion Criteria:

          -  Is able to provide written informed consent prior to study entry

          -  Is male or female, 18 - 85 years of age

          -  Has a diagnosis of postherpetic neuralgia that has been present for at least 3 months
             since the resolution of the skin rash (shingles), and has been associated with at
             least moderate pain

          -  Has a body mass index (BMI) between 17 and 36, inclusive

          -  Has on average postherpetic neuralgia pain severity of at least "4" on the 11-point
             NPRS-12 scale over three days prior to the Treatment Visit.

          -  At the Treatment Visit, entry into the study for dosing will require a baseline score
             of 4 or greater on the following 'Numerical Pain Rating Scale' (NPRS-NOW): "How would
             you rate your pain RIGHT NOW using a zero to ten scale, where zero equals no pain and
             ten is the worst pain you can imagine." If the subject fails to qualify for the
             Treatment Visit because of a baseline pain score below 4, he or she may return on any
             day within a fourteen day period to attempt to qualify again. A subject will be
             allowed a maximum of two reassessments to qualify on the basis of the NPRS-NOW scale.

          -  Female subjects must be of non childbearing potential (defined as postmenopausal for
             at least 1 year or surgically sterile [bilateral tubal ligation, bilateral
             oophorectomy or hysterectomy]) or must be using adequate contraception (practicing one
             of the following methods of birth control):

          -  Total abstinence from sexual intercourse (minimum of one complete menstrual cycle
             before study entry),

          -  A partner who is physically unable to impregnate the subject (e.g., vasectomized)

          -  Contraceptives (oral, parenteral, or transdermal) for 3 consecutive months prior to
             study drug administration,

          -  Intrauterine device (IUD), or

          -  Double barrier method (condoms, sponge, diaphragm, or vaginal ring with spermicidal
             jellies or cream)

          -  If female of childbearing potential, subject must have a negative serum pregnancy test
             at screening

          -  Able to communicate meaningfully with the study observer and staff

          -  No known allergies to study medication

        Exclusion Criteria:

          -  Has another source of moderate-to-severe pain apart from the postherpetic neuralgia
             that might be confused with the PHN pain

          -  Is actively abusing alcohol or drugs

          -  Is unable to refrain from alcohol for a period beginning 24 hours prior to the
             treatment visit until the end of the study

          -  Is scheduled to undergo any surgical procedures during the period of study duration

          -  Has a history of any active serious medical conditions including cancer (with the
             exception of benign uterine dysplasia or removed skin carcinomas), cardiovascular,
             respiratory, renal, hepatic, gastrointestinal, endocrine, immunologic, hematologic,
             neurologic or psychiatric disease that would contraindicate study participation

          -  Has moderate to severe (New York Heart Association [NYHA] Class 3 or 4) heart failure
             defined as heart failure which significantly limits physical activity by provoking
             fatigue, palpitations or dyspnea.

          -  Has a history of either type 1 or type 2 diabetes mellitus

          -  Has taken a fixed scheduled opioid regimen within 3 days prior to the Treatment Visit.
             A fixed scheduled regimen of another type of analgesic, e.g., nonsteroidal
             antiinflammatory drug (NSAID) or an adjuvant analgesic will be allowed as long as the
             dose and schedule of administration were not changed for at least 2 weeks prior to
             dosing.

          -  Has used a short-acting "as needed" opioid less than 12 hours prior to dosing or an
             "as needed" NSAID dose less than 24 hours prior to dosing

          -  Has used extended duration oral analgesics up to 48 hours prior to the Treatment Visit

          -  Has applied lidocaine patches or dermal analgesics within 7 days prior to the
             Treatment Visit

          -  Has received an anesthetic block within two weeks of the Screening Visit

          -  Has received any prior neurolytic nerve block in the area of the PHN pain

          -  Is taking tricyclic, selective serotonin reuptake inhibitor (SSRI) or serotonin and
             noradrenaline reuptake inhibitor (SNRI) antidepressants for PHN (or for indications
             other than pain) and the dosage has been changed within 14 days of the Treatment
             Visit. Only subjects on stable doses from at least 14 days prior to the Treatment
             Visit through the duration of the study will be eligible to participate

          -  Is taking gabapentin (Neurontin), pregabalin (Lyrica), or duloxetine (Cymbalta) and
             the dosage has been changed within 14 days of the Treatment Visit. Only subjects
             receiving stable doses for at least 14 days prior to the Treatment Visit and are
             willing to continue taking the same doses for the duration of the study will be
             eligible to participate

          -  Has taken any medication that is a substrate of the cytochrome P450 enzyme CYP2C9
             within 4 days of dosing with study drug or is unwilling to refrain from such
             medications through the course of study drug treatment

          -  Has taken any prescription or over-the-counter medication within three days prior to
             the Treatment Visit, or herbal agents or other nutraceutical products within 14 days
             prior to the Treatment Visit, that in the opinion of the Investigator would be
             expected to confound the analgesic response

          -  Has documented liver failure or a serum ALT, AST, alkaline phosphatase, or GGT greater
             than 2.5 times the upper limit of normal, or total bilirubin greater than 1.5 times
             the upper limit of normal without a known, not clinically significant explanation

          -  Has a Brain Natriuretic Peptide (BNP) level > 150 pg/mL

          -  Has a history of poorly controlled hyperthyroidism or hypothyroidism or Thyroid
             Stimulating Hormone (TSH) levels that are < 0.3 or > 5.5 µlU/mL

          -  Has moderate or severe renal failure defined as a calculated creatinine clearance of <
             60mL/min from the Cockcroft & Gault formula

          -  Has a clinically significant abnormality on 12-lead electrocardiogram

          -  Has a known history of a positive Human Immunodeficiency Virus (HIV) antibody test or
             known HIV infection

          -  Has a history of a positive Hepatitis B core antibody, or anti-HCV antibody test

          -  Has previously been admitted to this study

          -  Has received an investigational medication within 30 days prior to the Treatment Visit