MedPath

A Study to Evaluate the Safety and Efficacy of Relugolix in Men With Advanced Prostate Cancer

Phase 3
Completed
Conditions
Prostate Cancer
Interventions
Registration Number
NCT03085095
Lead Sponsor
Myovant Sciences GmbH
Brief Summary

The purpose of this study is to determine the efficacy and safety of relugolix 120 milligrams (mg) orally once daily for 48 weeks on maintaining serum testosterone suppression to castrate levels (\< 50 nanograms/deciliter \[ng/dL\]) in participants with androgen-sensitive advanced prostate cancer.

Detailed Description

This is a phase 3, multinational, randomized, open-label, parallel group study to evaluate the efficacy and safety of oral daily relugolix 120 mg in participants with androgen-sensitive advanced prostate cancer who require at least 1 year of continuous androgen-deprivation therapy. Relugolix 120 mg orally once daily or leuprolide acetate depot suspension, 22.5 mg (or 11.25 mg in Japan and Taiwan based on local labels), every 3 months by subcutaneous injection will be administered to participants.

There are 2 analyses for this study, a primary analysis and a final analysis.

Primary Analysis:

The primary analysis of efficacy and safety has been completed (N=934). Participants were randomized 2:1 to receive relugolix or leuprolide for 48 weeks, followed by a 30-day safety follow-up visit or early termination 30-day safety follow-up.

Final Analysis:

The final analysis will occur after additional participants with metastatic disease (approximately 130) have been enrolled and randomized from any sites to the study, and have completed the 48-week treatment period. A cohort of participants enrolled in China and Taiwan will be analyzed separately once they have completed treatment to support registration in China.

Eligible participants were randomized 2:1 to relugolix or leuprolide arm and will attend visits monthly (every 4 weeks) where serum testosterone and prostate-specific antigen will be assessed. Safety will be assessed throughout the study by monitoring adverse events, vital signs, physical examinations, clinical laboratory tests, and 12-lead electrocardiograms.

Castration resistance-free survival will be assessed up to Week 49, Day 1 of the study and reported as part of the final analysis.

The study enrolled 1134 participants, including 139 participants with metastatic advanced prostate cancer to support the analysis of the secondary endpoint of castration resistance-free survival and 93 Chinese participants (enrolled in China and Taiwan) to support registration in China.

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
1134
Inclusion Criteria
  1. Has histologically or cytologically confirmed diagnosis of adenocarcinoma of the prostate.

  2. Is a candidate for, in the opinion of the investigator, at least 1 year of continuous androgen deprivation therapy for the management of androgen-sensitive advanced prostate cancer with 1 of the following clinical disease state presentations:

    1. Evidence of biochemical (PSA) or clinical relapse following local primary intervention with curative intent, such as surgery, radiation therapy, cryotherapy, or high-frequency ultrasound and not a candidate for salvage treatment by surgery; or
    2. Newly diagnosed androgen-sensitive metastatic disease; or
    3. Advanced localized disease unlikely to be cured by local primary intervention with either surgery or radiation with curative intent.
  3. Has a serum testosterone at the Screening visit of ≥ 150 ng/dL (5.2 nanomoles [nmol]/liter [L]).

  4. Has a serum PSA concentration at the Screening visit of > 2.0 ng/milliliter (mL) (2.0 microgram [μg]/L), or, when applicable, post radical prostatectomy of > 0.2 ng/mL (0.2 μg/L) or post radiotherapy, cryotherapy, or high frequency ultrasound > 2.0 ng/mL (2.0 μg/L) above the post interventional nadir.

  5. Has an Eastern Cooperative Oncology Group performance status of 0 or 1 at initial screening and at baseline.

Key

Exclusion Criteria
  1. In the investigator's opinion, is likely to require chemotherapy or surgical therapy for symptomatic disease management within 2 months of initiating androgen deprivation therapy.
  2. Previously received gonadotropin-releasing hormone analog or other form of androgen deprivation therapy (estrogen or antiandrogen) for > 18 months total duration. If androgen deprivation therapy was received for ≤ 18 months total duration, then that therapy must have been completed at least 3 months prior to baseline. If the dosing interval of the depot is longer than 3 months, then the prior androgen deprivation therapy must have been completed at least as long as the dosing interval of the depot.
  3. Previous systemic cytotoxic treatment for prostate cancer (for example, taxane-based regimen).
  4. Metastases to brain per prior clinical evaluation.
  5. Participants with myocardial infarction, unstable symptomatic ischemic heart disease, cerebrovascular events, or any significant cardiac condition within the prior 6 months.
  6. Active conduction system abnormalities.
  7. Uncontrolled hypertension.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Leuprolide AcetateLeuprolide AcetateLeuprolide acetate for 48 weeks
RelugolixRelugolixRelugolix for 48 weeks
Primary Outcome Measures
NameTimeMethod
Sustained Castration RateFrom Week 5 Day 1 (Day 29) to Week 49 Day 1 (Day 337)

Sustained castration rate defined as the cumulative probability of testosterone suppression to \< 50 nanogram (ng)/deciliter (dL). The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.

The lower bound of the 95% confidence interval (CI) for the cumulative probability of sustained testosterone suppression in the relugolix treatment group must have been ≥ 90% to meet evaluation criteria for efficacy.

Secondary Outcome Measures
NameTimeMethod
Change From Baseline In QoL Total Score As Assessed By The EORTC-QLQ-PR25 Sexual Activity And Functioning And Hormonal-Treatment-Related Symptom SubdomainsBaseline, Week 49 Day 1 (Day 337)

Subscales for assessment of hormonal treatment-related symptoms (6 items) and sexual activity and function (6 items) from the EORTC-QLQ-PR25 25-item prostate cancer module of the EORTC are presented. Questions used 4 point scale (1 'Not at all' to 4 'Very much'). All raw domain scores are linearly transformed to a 0-100 scale. An increase in activity or functioning scores indicates improvement (higher/healthier level of functioning) and a decrease in symptom scores indicates improvement (lower level of symptoms/problems).

Change From Baseline In QoL Total Score As Assessed By The European Quality Of Life 5-Dimension 5-Level Questionnaire (EuroQoL EQ-5D-5L)Baseline, Week 49 Day 1 (Day 337)

The EuroQoL EQ-5D-5L comprises 5 dimensions (mobility, self-care, usual activities, pain/discomfort, and anxiety/depression). Each dimension has 5 levels: no problems (1 as numerical score), slight problems (2 as numerical score), moderate problems (3 as numerical score), severe problems (4 as numerical score), and extreme problems (5 as numerical score). The total score ranges from 0 to 100. A decrease in score indicates improvement.

Percent Change From Baseline In Serum Concentrations Of FSHWeek 1 Day 4 (Day 4), Week 5 Day 1 (Day 29), Week 25 Day 1 (Day 169), and Week 49 Day 1 (Day 337)

Blood samples were collected from participants for hormonal measurements.

Percent Change From Baseline In Serum Concentrations Of Sex Hormone-Binding GlobulinWeek 5 Day 1 (Day 29), Week 25 Day 1 (Day 169), and Week 49 Day 1 (Day 337)

Blood samples were collected from participants for hormonal measurements.

Maximum Observed Plasma Concentration (Cmax) Of RelugolixPredose and 0.5, 1, 2, 4, 6, 8, 12, and 24 hours postdose on Day 1 and Week 2

The Cmax of relugolix was determined for single and repeat doses in subsets of participants from Japan. Single dose pharmacokinetics (PK) was assessed on Day 1 following an initial 360 mg dose of relugolix. Repeat dose PK was assessed following repeat dosing of relugolix 120 mg once daily for 2 weeks.

Profound Castration Rate At Week 3 Day 1 (Day 15)Week 3 Day 1 (Day 15)

Castration rate defined as the cumulative probability of testosterone suppression to \< 20 ng/dL. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.

PSA Response Rate At Week 3 Day 1Week 3 Day 1 (Day 15)

PSA response defined as \> 50% reduction in PSA from baseline. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.

PSA Response Rate At Week 5 Day 1Week 5 Day 1 (Day 29)

PSA response defined as \> 50% reduction in PSA from baseline. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.

Testosterone Recovery RateDay 90 follow-up

The cumulative probability of testosterone recovery back to \> 280 ng/dL (lower limit of the normal range), back to ≥ 50 ng/dL (definition of castration), and back to \> 280 ng/dL or baseline at 90 days after drug discontinuation was assessed. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.

Sustained Profound Castration Rate From Week 5 Day 1 Through Week 49 Day 1Week 5 Day 1 (Day 29) through Week 49 Day 1 (Day 337)

Sustained profound castration rate was defined as the cumulative probability of testosterone suppression to \< 20 ng/dL. The rate was estimated by the Kaplan-Meier method and reported as percentage of participants.

Undetectable PSA RateWeek 25 Day 1 (Day 169)

Defined as the proportion of participants with PSA concentration \< 0.02 ng/milliliter (mL).The rate was estimated by the Kaplan-Meier method and reported as percentage of participants.

Rate Of PSA Progression-free SurvivalWeek 49 Day 1 (Day 337)

PSA progression was defined as the first increase in PSA of 25% or greater and 2 ng/mL or greater above the nadir with confirmation by a second consecutive PSA measurement at least 3 weeks later. For participants without declining PSA from baseline, a PSA increase of ≥ 25% and ≥ 2 ng/mL from baseline beyond 12 weeks was considered PSA progression. The rate of progression-free survival was estimated using the Kaplan-Meier method and reported as percentage of participants.

Percent Change From Baseline In Serum Concentrations Of Luteinizing HormoneWeek 1 Day 4 (Day 4), Week 5 Day 1 (Day 29), Week 25 Day 1 (Day 169), and Week 49 Day 1 (Day 337)

Blood samples were collected from participants for hormonal measurements.

Area Under The Concentration-Time Curve (AUC0-τ) Of RelugolixPredose and 0.5, 1, 2, 4, 6, 8, 12, and 24 hours postdose on Day 1 and Week 2

The AUC0-τ of relugolix was determined for single and repeat doses in subsets of participants from Japan. Single dose PK was assessed on Day 1 following an initial 360 mg dose of relugolix. Repeat dose PK was assessed following repeat dosing of relugolix 120 mg once daily for 2 weeks.

Castration Rate At Week 1 Day 4Week 1 Day 4 (Day 4)

Castration rate was defined as the cumulative probability of testosterone suppression to \< 50 ng/dL. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.

Confirmed Prostate-specific Antigen (PSA) Response RateWeek 3 Day 1 (Day 15) and Week 5 Day 1 (Day 29)

Confirmed PSA response defined as \> 50% reduction in PSA from baseline at Week 3 Day 1 followed with confirmation at Week 5 Day 1.

Castration Rate At Week 3 Day 1Week 3 Day 1 (Day 15)

Castration rate was defined as the cumulative probability of testosterone suppression to \< 50 ng/dL. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.

Follicle-stimulating Hormone (FSH) LevelWeek 25 Day 1 (Day 169)

To evaluate the effect of relugolix and leuprolide acetate on FSH suppression.

Profound Castration Rate At Week 1 Day 4 (Day 4)At Week 1 Day 4 (Day 4)

Castration rate defined as the cumulative probability of testosterone suppression to \< 20 ng/dL. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.

Change From Baseline In Quality Of Life (QoL) Total Score As Assessed By The Global Health Domain Of The European Organisation Of Research And Treatment Of Cancer (EORTC)-Quality Of Life Questionnaire (QLQ)-C30Baseline, Week 49 Day 1 (Day 337)

The EORTC QLQ-C30 core measurement was used to capture distal outcomes, including physical, social functioning, and overall health-related quality of life. The questionnaire incorporates 30 questions comprising nine multi-item scales: 5 functional scales (physical, role, cognitive, emotional, and social); 3 symptom scales (fatigue, pain, and nausea and vomiting); and a global health and quality of life scale. All raw domain scores are linearly transformed to a 0-100 scale. The global health and quality of life domain is presented. An increase in activity or functioning scores indicates improvement (higher/healthier level of functioning) and a decrease in symptom scores indicates improvement (lower level of symptoms/problems).

Change From Baseline In QoL Total Score For Remaining Domain Scores As Assessed By The EORTC-QLQ-C30Baseline, Week 49 Day 1 (Day 337)

The EORTC QLQ-C30 core measurement was used to capture distal outcomes, including physical, social functioning, and overall health-related quality of life. The questionnaire incorporates 30 questions comprising nine multi-item scales: 5 functional scales (physical, role, cognitive, emotional, and social); 3 symptom scales (fatigue, pain, and nausea and vomiting); and a global health and quality of life scale. All raw domain scores are linearly transformed to a 0-100 scale. All domains except for the global health and quality are presented. An increase in activity or functioning scores indicates improvement (higher/healthier level of functioning) and a decrease in symptom scores indicates improvement (lower level of symptoms/problems).

Change From Baseline In QoL Total Score For Urinary And Bowel Symptoms Domains As Assessed By The EORTC-QLQ-PR25Baseline, Week 49 Day 1 (Day 337)

Subscale assessments of urinary symptoms (9 items) and bowel symptoms (4 items) from the EORTC-QLQ-PR25 25-item prostate cancer module of the EORTC are presented. Questions used 4 point scale (1 'Not at all' to 4 'Very much'). All raw domain scores are linearly transformed to a 0-100 scale. A decrease in symptom scores indicates improvement (lower level of symptoms/problems).

Time To Maximum Observed Plasma Concentration (Tmax) Of RelugolixPredose and 0.5, 1, 2, 4, 6, 8, 12, and 24 hours postdose on Day 1 and Week 2

The Tmax of relugolix was determined for single and repeat doses in subsets of participants from Japan. Single dose PK was assessed on Day 1 following an initial 360 mg dose of relugolix. Repeat dose PK was assessed following repeat dosing of relugolix 120 mg once daily for 2 weeks.

Sustained Profound Castration Rate From Week 25 Day 1 Through Week 49 Day 1Week 25 Day 1 (Day 169) through Week 49 Day 1 (Day 337)

Sustained profound castration rate was defined as the cumulative probability of testosterone suppression to \< 20 ng/dL. The rate was estimated by the Kaplan-Meier method and reported as percentage of participants.

Percent Change From Baseline In Serum Concentrations Of DihydrotestosteroneWeek 5 Day 1 (Day 29), Week 25 Day 1 (Day 169), and Week 49 Day 1 (Day 337)

Blood samples were collected from participants for hormonal measurements.

Trial Locations

Locations (149)

Greensboro

🇺🇸

Greensboro, North Carolina, United States

Albany

🇺🇸

Albany, New York, United States

Syracuse

🇺🇸

Syracuse, New York, United States

Camperdown

🇦🇺

Camperdown, New South Wales, Australia

Las Vegas

🇺🇸

Las Vegas, Nevada, United States

Durham

🇺🇸

Durham, North Carolina, United States

San Antonio

🇺🇸

San Antonio, Texas, United States

Lanzhou

🇨🇳

Lanzhou, China

Linz

🇦🇹

Linz, Austria

Strasbourg

🇫🇷

Strasbourg, Bas-Rhin, France

Chiba

🇯🇵

Chiba, Japan

Amsterdam

🇳🇱

Amsterdam, Noord Holland, Netherlands

Nakano-ku

🇯🇵

Nakano-ku, Tokyo, Japan

Exeter

🇬🇧

Exeter, Devon, United Kingdom

Itabuna

🇧🇷

Itabuna, Bahia, Brazil

Quebec

🇨🇦

Quebec, Canada

Salvador

🇧🇷

Salvador, Bahia, Brazil

Hamilton

🇳🇿

Hamilton, New Zealand

Porto Alegre

🇧🇷

Porto Alegre, Rio Grande Do Sul, Brazil

Ijuí

🇧🇷

Ijuí, Rio Grande Do Sul, Brazil

Passo Fundo

🇧🇷

Passo Fundo, Rio Grande Do Sul, Brazil

Shanghai

🇨🇳

Shanghai, China

Nashville

🇺🇸

Nashville, Tennessee, United States

Orange

🇺🇸

Orange, California, United States

Sala

🇸🇰

Šaľa, Slovakia

Tokyo

🇯🇵

Tokyo, Japan

Goyang-Si

🇰🇷

Goyang-si, Gyeonggido, Korea, Republic of

Helsinki

🇫🇮

Helsinki, Finland

Tampere

🇫🇮

Tampere, Finland

Suzhou

🇨🇳

Suzhou, China

Aarhus

🇩🇰

Aarhus, Denmark

Milano

🇮🇹

Milano, Italy

Turku

🇫🇮

Turku, Finland

Meldola

🇮🇹

Meldola, Emilia-Romagna, Italy

Braunschweig

🇩🇪

Braunschweig, Niedersachsen, Germany

Sumida-ku

🇯🇵

Sumida-ku, Tokyo, Japan

Seoul

🇰🇷

Seoul, Korea, Republic of

Creteil

🇫🇷

Créteil, Val-de-Marne, France

Suita

🇯🇵

Suita, Osaka, Japan

Alborg

🇩🇰

Aalborg, Denmark

Herlev

🇩🇰

Herlev, Denmark

Lyon

🇫🇷

Lyon, France

Hangzhou

🇨🇳

Hangzhou, China

Vejle

🇩🇰

Vejle, Denmark

Pierre Benite

🇫🇷

Pierre-Bénite, Rhone, France

Seinajoki

🇫🇮

Seinäjoki, Finland

A Coruna

🇪🇸

A Coruña, A Coruna, Spain

Gdynia

🇵🇱

Gdynia, Pomorskie, Poland

Kosice

🇸🇰

Košice, Slovakia

Candiolo

🇮🇹

Candiolo, Piemonte, Italy

Orbassano

🇮🇹

Orbassano, Piemonte, Italy

Dunedin

🇳🇿

Dunedin, New Zealand

Madrid

🇪🇸

Madrid, Spain

Munster

🇩🇪

Münster, Germany

Cremona

🇮🇹

Cremona, Lombardia, Italy

Arezzo

🇮🇹

Arezzo, Toscana, Italy

Fukuoka

🇯🇵

Fukuoka, Japan

Hiroshima

🇯🇵

Hiroshima, Japan

Kita-gun

🇯🇵

Kita, Japan

Maebashi

🇯🇵

Maebashi, Japan

Nagasaki

🇯🇵

Nagasaki, Japan

Christchurch

🇳🇿

Christchurch, New Zealand

Daegu

🇰🇷

Daegu, Korea, Republic of

Busan

🇰🇷

Busan, Korea, Republic of

Kyoto

🇯🇵

Kyoto, Japan

Lublin

🇵🇱

Lublin, Lubelskie, Poland

Nottingham

🇬🇧

Nottingham, United Kingdom

Rhyl

🇬🇧

Rhyl, United Kingdom

Trencin

🇸🇰

Trenčín, Slovakia

Barcelona

🇪🇸

Barcelona, Spain

Valencia

🇪🇸

Valencia, Spain

Stockholm

🇸🇪

Stockholm, Sodermandlands Ian, Sweden

Malmo

🇸🇪

Malmö, Sweden

Salamanca

🇪🇸

Salamanca, Spain

Scunthorpe

🇬🇧

Scunthorpe, North Lincolnshire, United Kingdom

Taipei

🇨🇳

Taipei, Taiwan

Orebro

🇸🇪

Örebro, Orebro Ian, Sweden

Denver

🇺🇸

Denver, Colorado, United States

Omaha

🇺🇸

Omaha, Nebraska, United States

Oklahoma City

🇺🇸

Oklahoma City, Oklahoma, United States

Hwasun

🇰🇷

Hwasun, Korea, Republic of

Planegg

🇩🇪

Planegg, Bayern, Germany

Emmendingen

🇩🇪

Emmendingen, Baden-Wurttemberg, Germany

Dresden

🇩🇪

Dresden, Germany

Lubeck

🇩🇪

Lübeck, Germany

Tauranga

🇳🇿

Tauranga, New Zealand

Cincinnati

🇺🇸

Cincinnati, Ohio, United States

Pompano Beach

🇺🇸

Pompano Beach, Florida, United States

Baltimore

🇺🇸

Baltimore, Maryland, United States

Troy

🇺🇸

Troy, Michigan, United States

Garden City

🇺🇸

Garden City, New York, United States

Plainview

🇺🇸

Plainview, New York, United States

Poughkeepsie

🇺🇸

Poughkeepsie, New York, United States

Lancaster

🇺🇸

Lancaster, Pennsylvania, United States

Middleburg Heights

🇺🇸

Middleburg Heights, Ohio, United States

Myrtle Beach

🇺🇸

Myrtle Beach, South Carolina, United States

Tweed Heads

🇦🇺

Tweed Heads, New South Wales, Australia

Wahroonga

🇦🇺

Wahroonga, New South Wales, Australia

Kortrijk

🇧🇪

Kortrijk, Belgium

Redcliffe

🇦🇺

Redcliffe, Queensland, Australia

Southport

🇦🇺

Southport, Queensland, Australia

Teresina

🇧🇷

Teresina, Piauí, Brazil

Natal

🇧🇷

Natal, Rio Grande Do Norte, Brazil

Changchun

🇨🇳

Chang chun, Jilin, China

Joinville

🇧🇷

Joinville, Santa Catarina, Brazil

Curitiba

🇧🇷

Curitiba, Brazil

São José Do Rio Preto

🇧🇷

São José Do Rio Preto, Sao Paulo, Brazil

Calgary

🇨🇦

Calgary, Alberta, Canada

Halifax

🇨🇦

Halifax, Nova Scotia, Canada

Vancouver

🇨🇦

Vancouver, British Columbia, Canada

Montreal

🇨🇦

Montréal, Quebec, Canada

London

🇨🇦

London, Ontario, Canada

Nanjing

🇨🇳

Nanjing, Jiangsu, China

Beijing

🇨🇳

Beijing, China

Taiyuan

🇨🇳

Taiyuan, Shanxi, China

Beijing Shi

🇨🇳

Beijing, China

Chongqing

🇨🇳

Chongqing, China

Nanchang

🇨🇳

Nanchang, China

Uppsala

🇸🇪

Uppsala, Uppsala Lan, Sweden

Sneek

🇳🇱

Sneek, Netherlands

Katowice

🇵🇱

Katowice, Poland

Brick

🇺🇸

Brick, New Jersey, United States

Brussels

🇧🇪

Brussels, Belgium

Bratislava

🇸🇰

Bratislava, Slovakia

Poprad

🇸🇰

Poprad, Slovakia

Gent

🇧🇪

Gent, Oost-Vlaanderen, Belgium

Yokohama

🇯🇵

Yokohama, Kanagawa, Japan

Osaka

🇯🇵

Osaka, Japan

Sapporo

🇯🇵

Sapporo, Japan

Tucson

🇺🇸

Tucson, Arizona, United States

Bunkyō-Ku

🇯🇵

Bunkyō-Ku, Tokyo, Japan

Ube

🇯🇵

Ube, Japan

Eindhoven

🇳🇱

Eindhoven, Noord Brabant, Netherlands

Nitra

🇸🇰

Nitra, Slovakia

Presov

🇸🇰

Prešov, Slovakia

Sherbrooke

🇨🇦

Sherbrooke, Quebec, Canada

Kanazawa-shi

🇯🇵

Kanazawa-shi, Isikawa, Japan

Sendai

🇯🇵

Sendai, Miyagi, Japan

Osaka-sayama

🇯🇵

Ōsaka-sayama, Osaka, Japan

Siedlce

🇵🇱

Siedlce, Mazowieckie, Poland

Kaohsiung City

🇨🇳

Kaohsiung City, Taiwan

Rome

🇮🇹

Rome, Lazio, Italy

Warszawa

🇵🇱

Warszawa, Mazowieckie, Poland

Martin

🇸🇰

Martin, Slovakia

Oviedo

🇪🇸

Oviedo, Asturias, Spain

Des Moines

🇺🇸

Des Moines, Iowa, United States

Wichita

🇺🇸

Wichita, Kansas, United States

Albuquerque

🇺🇸

Albuquerque, New Mexico, United States

Jeffersonville

🇺🇸

Jeffersonville, Indiana, United States

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