Relistor Drug Information
Generic name: METHYLNALTREXONE BROMIDE
Uses of Relistor
Opioid-Induced Constipation in Adult Patients with Chronic Non-Cancer Pain RELISTOR tablets and RELISTOR injection are indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dosage escalation.
Opioid-Induced Constipation in Adult Patients with Advanced Illness RELISTOR injection is indicated for the treatment of OIC in adult patients with advanced illness or pain caused by active cancer who require opioid dosage escalation for palliative care.
Dosage & Administration of Relistor
Important Administration Information •
Be within close proximity to toilet facilities once RELISTOR is administered. • Discontinue RELISTOR if treatment with the opioid pain medication is also discontinued. • In adult patients with chronic non-cancer pain and OIC: o Patients receiving opioids for less than 4 weeks may be less responsive to RELISTOR. o Discontinue all maintenance laxative therapy prior to initiation of RELISTOR. Laxative(s) can be used as needed if there is a suboptimal response to RELISTOR after three days. o Re-evaluate the continued need for RELISTOR when the opioid regimen is changed to avoid adverse reactions. o In patients with chronic non-cancer pain and OIC, take RELISTOR tablets with water on an empty stomach at least 30 minutes before the first meal of the day.
Opioid-Induced Constipation in Adult Patients with Chronic Non-Cancer Pain • The recommended dosage of RELISTOR tablets is 450 mg taken orally once daily in the morning. • The recommended dosage of RELISTOR injection is 12 mg administered subcutaneously once daily.
Opioid-Induced Constipation in Adult Patients with Advanced Illness The pre-filled syringe is only for patients who require a RELISTOR injection dose of 8 mg or 12 mg. Use the vial for patients who require other doses of RELISTOR injection. Table 1 below shows the recommended weight-based dose of RELISTOR injection and the corresponding injection volume.
The recommended dosage regimen is one dose administered subcutaneously every other day, as needed. Do not administer more frequently than one dose per 24-hour period.
Dosage in Patients with Hepatic Impairment OIC in Adult Patients with Chronic Non-Cancer Pain • RELISTOR tablets: The recommended dosage in adult patients with moderate or severe hepatic impairment (Child-Pugh Class B or C) is 150 mg, once daily in the morning. • RELISTOR injection: If considering dose adjustment for patients with severe hepatic impairment, follow the recommendations in Table 3. Calculate the injection volume for these patients by multiplying the patient weight in kilograms by 0.00375 and then rounding up the volume to the nearest 0.1 mL.
Preparation and Administration of RELISTOR Injection •
- RELISTOR injection is for subcutaneous use only. • Single-dose pre-filled syringes: Do not remove the pre-filled syringe from the tray until ready to administer. • Inspect RELISTOR injection visually for particulate matter and discoloration prior to administration. RELISTOR injection is colorless to pale yellow. Discard the pre-filled syringe or vial if particulate matter or discoloration is present. • Administer RELISTOR injection subcutaneously in the upper arm, abdomen or thigh. Do not inject at the same spot each time (rotate injection sites). • RELISTOR single-dose vials: Once drawn into the syringe, if immediate administration is not possible, store at ambient room temperature and administer within 24 hours. Discard any unused portion that remains in the vial. • For patient or caregiver instructions for preparation and administration of RELISTOR injection (including recommended specifications for the syringe and needle to be used with the single-dose vial), see Instructions for Use.
| Table 1: Weight-Based Dosing of RELISTOR Injection and Corresponding Injection Volume for Adult Patients with OIC and Advanced Illness | ||
| Weight of Adult Patient | Subcutaneous Dose | Injection Volume |
| Less than 38 kg | 0.15 mg/kg | See below* |
| 38 kg to less than 62 kg | 8 mg | 0.4 mL |
| 62 kg to 114 kg | 12 mg | 0.6 mL |
| More than 114 kg | 0.15 mg/kg | See below* |
| *Calculate the injection volume for these patients by multiplying the patient weight in kilograms by 0.0075 and then rounding up the volume to the nearest 0.1 mL. | ||
| Table 2: Weight-Based Dosing in Moderate and Severe Renal Impairment of RELISTOR Injection and Corresponding Injection Volume for Adult Patients with OIC and Advanced Illness | ||
| Weight of Adult Patient | Subcutaneous Dose | Injection Volume |
| Less than 38 kg | 0.075 mg/kg | See below* |
| 38 kg to less than 62 kg | 4 mg | 0.2 mL |
| 62 kg to 114 kg | 6 mg | 0.3 mL |
| More than 114 kg | 0.075 mg/kg | See below* |
| Table 3: Weight-Based Dosing in Severe Hepatic Impairment of RELISTOR Injection and Corresponding Injection Volume for Adult Patients with OIC and Chronic Non-Cancer Pain | ||
| Weight of Adult Patient | Subcutaneous Dose | Injection Volume |
| Less than 38 kg | 0.075 mg/kg | See below* |
| 38 kg to less than 62 kg | 4 mg | 0.2 mL |
| 62 kg to 114 kg | 6 mg | 0.3 mL |
| More than 114 kg | 0.075 mg/kg | See below* |
| Table 1: Weight-Based Dosing of RELISTOR Injection and Corresponding Injection Volume for Adult Patients with OIC and Advanced Illness | ||
| Weight of Adult Patient | Subcutaneous Dose | Injection Volume |
| Less than 38 kg | 0.15 mg/kg | See below* |
| 38 kg to less than 62 kg | 8 mg | 0.4 mL |
| 62 kg to 114 kg | 12 mg | 0.6 mL |
| More than 114 kg | 0.15 mg/kg | See below* |
| *Calculate the injection volume for these patients by multiplying the patient weight in kilograms by 0.0075 and then rounding up the volume to the nearest 0.1 mL. | ||
| Table 2: Weight-Based Dosing in Moderate and Severe Renal Impairment of RELISTOR Injection and Corresponding Injection Volume for Adult Patients with OIC and Advanced Illness | ||
| Weight of Adult Patient | Subcutaneous Dose | Injection Volume |
| Less than 38 kg | 0.075 mg/kg | See below* |
| 38 kg to less than 62 kg | 4 mg | 0.2 mL |
| 62 kg to 114 kg | 6 mg | 0.3 mL |
| More than 114 kg | 0.075 mg/kg | See below* |
Side Effects of Relistor
Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Opioid-Induced Constipation in Adult Patients with Chronic Non-Cancer Pain The safety of RELISTOR tablets was evaluated in a double-blind, placebo-controlled trial in adult patients with OIC and chronic non-cancer pain receiving opioid analgesia. After 4 weeks of double-blind treatment administered once daily, patients continued 8 weeks of double-blind treatment on an as needed basis (but not more than once daily).
The most common adverse reactions in adult patients with OIC and chronic non-cancer pain receiving RELISTOR tablets are shown in Table 4. After 4 weeks of double-blind treatment, patients began an 8‑week open-label treatment period during which RELISTOR injection 12 mg subcutaneously was administered less frequently than the recommended dosage regimen of 12 mg once daily. The adverse reactions in the table below may reflect symptoms of opioid withdrawal. Adverse reactions occurring in at least 1% of patients receiving RELISTOR injection 12 mg subcutaneously once daily and at an incidence greater than placebo. Includes: abdominal pain, upper abdominal pain, lower abdominal pain, abdominal discomfort and abdominal tenderness During the 4-week double-blind period, in patients with OIC and chronic non-cancer pain that received RELISTOR every other day, there was a higher incidence of adverse reactions, including nausea as compared to daily RELISTOR dosing.
Use of RELISTOR injection 12 mg subcutaneously every other day is not recommended in patients with OIC and chronic non-cancer pain. The rates of discontinuation due to adverse reactions during the double-blind period (Study 2) were higher in the RELISTOR once daily (7%) than the placebo group (3%). Abdominal pain was the most common adverse reaction resulting in discontinuation from the double-blind period in the RELISTOR once daily group (2%).
The safety of RELISTOR injection was also evaluated in a 48-week, open-label, uncontrolled trial in 1034 adult patients with OIC and chronic non-cancer pain (Study 3). Patients were allowed to administer RELISTOR injection 12 mg subcutaneously less frequently than the recommended dosage regimen of 12 mg once daily, and took a median of 6 doses per week. The adverse reactions seen in this study were similar to those observed during the 4-week double-blind period of Study 2.
It is not possible to establish a relationship between these events and RELISTOR. Opioid-Induced Constipation in Adult Patients with Advanced Illness The safety of RELISTOR injection was evaluated in two, double-blind, placebo-controlled trials in adult patients with OIC and advanced illness receiving palliative care: Study 4 included a single-dose, double-blind, placebo-controlled period, whereas Study 5 included a 14-day multiple dose, double-blind, placebo-controlled period. The most common adverse reactions in adult patients with OIC and advanced illness receiving RELISTOR injection are shown in Table 6 below. Adverse reactions occurring in at least 5% of patients receiving all doses of RELISTOR injection (0.075, 0.15, and 0.3 mg/kg) and at an incidence greater than placebo Includes: abdominal pain, upper abdominal pain, lower abdominal pain, abdominal discomfort and abdominal tenderness The rates of discontinuation due to adverse reactions during the double-blind, placebo-controlled clinical trials (Study 4 and Study 5) were comparable between RELISTOR (1%) and placebo (2%).
Postmarketing Experience
The following adverse reactions have been identified during post-approval use of RELISTOR injection. Because reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate the frequency or establish a causal relationship to drug exposure. Gastrointestinal Perforation, cramping, vomiting General Disorders and Administration Site Disorders Diaphoresis, flushing, malaise, pain.
Cases of opioid withdrawal have been reported.
| Table 4: Adverse Reactions* in 4-Week Double-Blind, Placebo-Controlled Period of Clinical Study of RELISTOR Tablets in Adult Patients with OIC and Chronic Non-Cancer Pain (Study 1) | ||
| Adverse Reaction | RELISTOR Tablets n = 200 | Placebo n = 201 |
| Abdominal Pain | 14% | 10% |
| Diarrhea | 5% | 2% |
| Headache | 4% | 3% |
| Abdominal Distention | 4% | 2% |
| Vomiting | 3% | 2% |
| Hyperhidrosis | 3% | 1% |
| Anxiety | 2% | 1% |
| Muscle Spasms | 2% | 1% |
| Rhinorrhea | 2% | 1% |
| Chills | 2% | 0% |
| Table 5: Adverse Reactions* in 4-Week Double-Blind, Placebo-Controlled Period of Clinical Study of RELISTOR Injection in Adult Patients with OIC and Chronic Non-Cancer Pain (Study 2) | ||
| Adverse Reaction | RELISTOR Injection n = 150 | Placebo n = 162 |
| Abdominal Pain* | 21% | 7% |
| Nausea | 9% | 6% |
| Diarrhea | 6% | 4% |
| Hyperhidrosis | 6% | 1% |
| Hot Flush | 3% | 2% |
| Tremor | 1% | <1% |
| Chills | 1% | 0% |
| Table 6: Adverse Reactions from All Doses in Double-Blind, Placebo-Controlled Clinical Studies of RELISTOR Injection in Adult Patients with OIC and Advanced Illness* (Studies 4 and 5) | ||
|---|---|---|
| Adverse Reaction | RELISTOR Injection n = 165 | Placebo n = 123 |
| Abdominal Pain | 29% | 10% |
| Flatulence | 13% | 6% |
| Nausea | 12% | 5% |
| Dizziness | 7% | 2% |
| Diarrhea | 6% | 2% |
| Table 4: Adverse Reactions* in 4-Week Double-Blind, Placebo-Controlled Period of Clinical Study of RELISTOR Tablets in Adult Patients with OIC and Chronic Non-Cancer Pain (Study 1) | ||
| Adverse Reaction | RELISTOR Tablets n = 200 | Placebo n = 201 |
| Abdominal Pain | 14% | 10% |
| Diarrhea | 5% | 2% |
| Headache | 4% | 3% |
| Abdominal Distention | 4% | 2% |
| Vomiting | 3% | 2% |
| Hyperhidrosis | 3% | 1% |
| Anxiety | 2% | 1% |
| Muscle Spasms | 2% | 1% |
| Rhinorrhea | 2% | 1% |
| Chills | 2% | 0% |
| Table 5: Adverse Reactions* in 4-Week Double-Blind, Placebo-Controlled Period of Clinical Study of RELISTOR Injection in Adult Patients with OIC and Chronic Non-Cancer Pain (Study 2) | ||
| Adverse Reaction | RELISTOR Injection n = 150 | Placebo n = 162 |
| Abdominal Pain* | 21% | 7% |
| Nausea | 9% | 6% |
| Diarrhea | 6% | 4% |
| Hyperhidrosis | 6% | 1% |
| Hot Flush | 3% | 2% |
| Tremor | 1% | <1% |
| Chills | 1% | 0% |
| Table 6: Adverse Reactions from All Doses in Double-Blind, Placebo-Controlled Clinical Studies of RELISTOR Injection in Adult Patients with OIC and Advanced Illness* (Studies 4 and 5) | ||
|---|---|---|
| Adverse Reaction | RELISTOR Injection n = 165 | Placebo n = 123 |
| Abdominal Pain | 29% | 10% |
| Flatulence | 13% | 6% |
| Nausea | 12% | 5% |
| Dizziness | 7% | 2% |
| Diarrhea | 6% | 2% |
Warnings & Cautions for Relistor
Gastrointestinal Perforation Cases of gastrointestinal perforation have been reported in adult patients with OIC and advanced illness with conditions that may be associated with localized or diffuse reduction of structural integrity in the wall of the gastrointestinal tract (e.g., peptic ulcer disease, Ogilvie’s syndrome, diverticular disease, infiltrative gastrointestinal tract malignancies or peritoneal metastases). Take into account the overall risk-benefit profile when using RELISTOR in patients with these conditions or other conditions which might result in impaired integrity of the gastrointestinal tract wall (e.g., Crohn’s disease). Monitor for the development of severe, persistent, or worsening abdominal pain; discontinue RELISTOR in patients who develop this symptom.
Severe or Persistent Diarrhea
If severe or persistent diarrhea occurs during treatment, advise patients to discontinue therapy with RELISTOR and consult their healthcare provider.
Opioid Withdrawal
Symptoms consistent with opioid withdrawal, including hyperhidrosis, chills, diarrhea, abdominal pain, anxiety, and yawning have occurred in patients treated with RELISTOR. Patients having disruptions to the blood-brain barrier may be at increased risk for opioid withdrawal and/or reduced analgesia. Monitor for adequacy of analgesia and symptoms of opioid withdrawal in such patients.
Drug Interactions with Relistor
Other Opioid Antagonists
Avoid concomitant use of RELISTOR with other opioid antagonists because of the potential for additive effects of opioid receptor antagonism and increased risk of opioid withdrawal.
Drugs Metabolized by Cytochrome P450 Isozymes
In healthy subjects, a subcutaneous dose of 0.3 mg/kg of RELISTOR did not significantly affect the metabolism of dextromethorphan, a CYP2D6 substrate.
Pregnancy Safety for Relistor
Pregnancy Risk Summary The limited available data with RELISTOR in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriages. There are clinical considerations when RELISTOR is used by pregnant women. In animal reproduction studies, no effects on embryofetal development were observed with the administration of intravenous methylnaltrexone bromide during organogenesis in rats and rabbits at doses up to 20 times and 26 times, respectively, the subcutaneous maximum recommended human dose (MRHD) of 12 mg RELISTOR injection per day.
The intravenous doses in rats and rabbits are about 0.5 times and 0.7 times, respectively, the oral MRHD of 450 mg/day. Advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is respectively. Clinical Considerations Fetal/Neonatal Adverse Reactions The use of RELISTOR during pregnancy may precipitate opioid withdrawal in a fetus due to the immature fetal blood-brain barrier. Data Animal Data Reproduction studies have been performed with methylnaltrexone bromide administered during the period of organogenesis to rats at intravenous doses up to 25 mg/kg/day (about 20 times the subcutaneous MRHD of 12 mg/day based on body surface area), and did not cause any adverse effects on embryofetal development.
In rabbits, intravenous doses of methylnaltrexone bromide up to 16 mg/kg/day (about 26 times the subcutaneous MRHD of 12 mg/day) did not show any embryofetal toxicity. A pre- and postnatal development study in rats showed no evidence of any adverse effect on pre- and postnatal development at subcutaneous doses of methylnaltrexone bromide up to 100 mg/kg/day (about 81 times the subcutaneous MRHD of 12 mg/day; about 2.2 times the oral MRHD of 450 mg/day).
Pediatric Use of Relistor
Pediatric Use Safety and effectiveness of RELISTOR tablets and injection have not been established in pediatric patients. Juvenile Animal Studies In juvenile rats administered intravenous methylnaltrexone bromide for 13 weeks, adverse clinical signs such as convulsions, tremors and labored breathing were observed, and the juvenile rats were found to be more sensitive to the adverse effects of methylnaltrexone when compared to adult animals. Juvenile dogs administered intravenous methylnaltrexone bromide for 13 weeks had a toxicity profile similar to adult dogs.
Contraindications for Relistor
RELISTOR is contraindicated in patients with known or suspected gastrointestinal obstruction and patients at increased risk of recurrent obstruction, due to the potential for gastrointestinal perforation.
Overdosage Information for Relistor
During clinical trials of RELISTOR administered orally and subcutaneously, one accidental case of methylnaltrexone bromide overdose was reported and no adverse events were reported as a result of the overdosage. A study of healthy subjects noted orthostatic hypotension associated with a dose of 0.64 mg/kg administered as an intravenous bolus. Monitor for signs or symptoms of orthostatic hypotension and initiate treatment as appropriate.
If a patient on opioid therapy receives an overdose of RELISTOR, the patient should be monitored closely for potential evidence of opioid withdrawal symptoms such as chills, rhinorrhea, diaphoresis or reversal of central analgesic effect. Base treatment on the degree of opioid withdrawal symptoms, including changes in blood pressure and heart rate, and on the need for analgesia.
Clinical Studies of Relistor
Opioid-Induced Constipation in Adult Patients with Chronic Non-Cancer Pain RELISTOR Tablets The efficacy of RELISTOR tablets in the treatment of OIC in patients with chronic non-cancer pain was evaluated in a randomized, double-blind, placebo-controlled study (Study 1). This study compared 4-week treatment of RELISTOR tablets 450 mg orally once daily with placebo. A total of 401 patients (200 RELISTOR, 201 placebo) were enrolled and treated in the double-blind period.
Patients had a history of chronic non-cancer pain for which they were taking opioids. The most common pain condition requiring opioid use was back pain. Other frequently reported primary pain conditions were arthritis, neurologic/neuropathic pain, joint/extremity pain, and fibromyalgia.
Prior to screening, patients were receiving opioid therapy for pain for 1 month or longer (median daily baseline oral morphine equivalent dose of 156 mg) and had OIC (less than 3 spontaneous bowel movements per week during the screening period). Constipation due to opioid use had to be associated with 1 or more of the following: A Bristol Stool Form Scale score of 1 or 2 for at least 25% of the bowel movements (BM), straining during at least 25% of the BMs or a sensation of incomplete evacuation after at least 25% of the BMs. Patients were required to be on a stable opioid regimen (daily dose 50 mg or more of oral morphine equivalents per day) a minimum of 2 weeks prior to the screening visit and received their opioid medication during the study as clinically needed.
The median duration of OIC at baseline was 53 months (4 years). Eligible patients were required to discontinue all previous laxative therapy and use only the study-permitted rescue laxative (bisacodyl tablets). If patients did not have a bowel movement for 3 consecutive days during the study, they were permitted to use rescue medication (up to 3 bisacodyl tablets taken orally once during a 24-hour period).
Bisacodyl tablets were taken 5 hours or longer and up to 8 hours after study drug administration. If rescue treatment with bisacodyl tablets did not result in a bowel movement, a second dose of bisacodyl or an enema 24 hours after rescue was permitted. Enema use was permitted after rescue with bisacodyl tablets had failed at least once.
A responder analysis was performed which defined the proportion of patients with 3 or more spontaneous bowel movements (SBMs)/week, with an increase of 1 or more SBM/week over baseline, for 3 or more out of the first 4 weeks of the treatment period. A SBM was defined as a bowel movement that occurred without laxative use during the previous 24 hours. Table 8 presents the proportion of patients who responded during the double-blind treatment period in the intent-to-treat (ITT) population, which included all randomized patients who received at least one dose of double-blind study medication.
CI = confidence interval; ITT = intent-to-treat; a Difference for active treatment vs. placebo; A responder is defined as a patient with 3 or more SBMs/week, with an increase of 1 or more SBM/week over baseline, for 3 or more out of the first 4 weeks of the treatment period. RELISTOR Injection The efficacy of RELISTOR injection in the treatment of OIC in patients with chronic non-cancer pain were evaluated in a randomized, double-blind, placebo-controlled study (Study 2). This study compared 4-week treatment of RELISTOR injection 12 mg administered subcutaneously once daily with placebo.
A total of 312 patients (150 RELISTOR, 162 placebo) were enrolled and treated in the double-blind period. The majority of patients had a primary diagnosis of back pain; other primary diagnoses included joint/extremity pain, fibromyalgia, neurologic/neuropathic pain, and rheumatoid arthritis. The median duration of OIC at baseline was 59 months (5 years).
The median patient age at baseline was 49 years, 62% were females and 90% were Caucasian. Rescue laxatives were prohibited until at least 4 hours after taking an injection of study medication. A responder analysis was performed which defined the proportion of patients with 3 or more (SBMs) per week for each of the 4 weeks of the double-blind period.
CI = confidence interval; mITT = modified intent-to-treat; a Difference for active treatment vs. placebo; A responder is defined as a patient with 3 or more SBMs per week for each of the 4 weeks in the double-blind period. b P-value for active treatment vs. placebo based on 2-sided Chi-square test. Following the first dose, 33% of patients in the RELISTOR treatment group had a SBM within 4 hours and approximately half of patients had a SBM prior to the second dose of RELISTOR injection.
Opioid-Induced Constipation in Adult Patients with Advanced Illness The efficacy of RELISTOR injection in the treatment of OIC in advanced illness patients receiving palliative care was demonstrated in two randomized, double-blind, placebo-controlled studies. In both studies, patients had advanced illness and received care to control their symptoms. The majority of patients had a primary diagnosis of incurable cancer; other primary diagnoses included end-stage COPD/emphysema, cardiovascular disease/heart failure, Alzheimer's disease/dementia, HIV/AIDS, or other advanced illnesses.
Prior to screening, patients had been receiving palliative opioid therapy (median daily baseline oral morphine equivalent dose of 172 mg), and had OIC (either less than 3 bowel movements in the preceding week or no bowel movement for 2 or more days). Patients were on a stable opioid regimen 3 or more days prior to randomization (not including PRN or rescue pain medication) and received their opioid medication during the study as clinically needed. Patients maintained their regular laxative regimen for at least 3 days prior to study entry, and throughout the study.
Rescue laxatives were prohibited from 4 hours before to 4 hours after taking an injection of study medication. Study 4 was a double-blind, placebo-controlled study which compared a single, subcutaneous dose of RELISTOR injection 0.15 mg/kg, and RELISTOR injection 0.3 mg/kg versus placebo. The double-blind dose was followed by an open-label 4-week dosing period, where RELISTOR injection could be used as needed, no more frequently than one dose in a 24-hour period.
Throughout both study periods, patients maintained their regular laxative regimen. The primary endpoint was the proportion of patients with a rescue-free laxation within 4 hours of the double-blind dose of study medication. Study 5 was a double-blind, placebo-controlled study which compared subcutaneous doses of RELISTOR injection given every other day for 2 weeks versus placebo.
Patients received opioid medication for at least 2 weeks prior to receiving study medication. During the first week Days patients received either 0.15 mg/kg RELISTOR injection or placebo. In the second week the patient's assigned dose could be increased to 0.3 mg/kg if the patient had 2 or fewer rescue-free laxations up to Day 8.
At any time, the patient's assigned dose could be reduced based on tolerability. Data from 133 (62 RELISTOR, 71 placebo) patients were analyzed. There were 2 primary endpoints: proportion of patients with a rescue-free laxation within 4 hours of the first dose of study medication and proportion of patients with a rescue-free laxation within 4 hours after at least 2 of the first 4 doses of study medication.
In both studies, in approximately 30% of patients, laxation was reported within 30 minutes of a dose of RELISTOR. Figure 1: Laxation Response within 4 Hours of the First Dose in Studies 4 and 5 In both studies, there was no evidence of differential effects of age or gender on safety or efficacy. No meaningful subgroup analysis could be conducted on race because the study population was predominantly Caucasian (88%).
Durability of Response Durability of response was explored in Study 5, and the laxation response rate was consistent from dose 1 through dose 7 over the course of the 2-week, double-blind period. During open-label treatment, patients maintained their regular laxative regimen. Laxation response was also explored in this open-label setting and appeared to be maintained over the course of 3 to 4 months of open-label treatment.
Opioid Use and Pain Scores No relationship between baseline opioid dose and laxation response in RELISTOR-treated patients was identified in exploratory analyses of these studies. In addition, median daily opioid dose did not vary meaningfully from baseline in either RELISTOR-treated patients or in placebo-treated patients. There were no clinically relevant changes in pain scores from baseline in either the RELISTOR or placebo-treated patients. figure1
| Table 8: Proportion of Responders* in the ITT Population in Study 1 of RELISTOR Tablets for the Treatment of OIC in Patients with Chronic Non-Cancer Pain | |||
| Treatment | N | n (%) | Percent Difference a (2-sided 95% CI) |
| RELISTOR Tablets 450 mg Once Daily | 200 | 103 (52%) | 13% (3%, 23%) |
| Placebo | 201 | 77 (38%) | |
| Table 9: Proportion of Responders* in the mITT Population in Study 2 of RELISTOR Injection for the Treatment of OIC in Patients with Chronic Non-Cancer Pain | ||||
| Treatment | N | n (%) | Percent Difference a (2-sided 95% CI) | P-value b |
| RELISTOR Injection 12 mg Once Daily | 150 | 88 (59%) | 20% (10%, 31%) | <0.001 |
| Placebo | 162 | 62 (38%) | ||
Drug information sourced from the FDA. This content is for informational purposes only and does not constitute medical advice. Consult a healthcare professional before making any medication decisions.
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