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Last Updated: February 7, 2025

CLINICAL TRIALS PROFILE FOR ROLAPITANT HYDROCHLORIDE


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All Clinical Trials for Rolapitant Hydrochloride

Trial ID Title Status Sponsor Phase Start Date Summary
NCT00394966 ↗ A Multicenter, Randomized, Controlled Trial of SCH 619734 for the Treatment of Chemotherapy-Induced Nausea and Vomiting (Study P04351AM2)(COMPLETED) Completed Schering-Plough Phase 2 2006-09-01 This is a Phase 2, randomized, multicenter, parallel-group, double-blind, placebo-controlled study of various doses of SCH 619734 in subjects receiving cisplatin-based chemotherapy. Ondansetron and dexamethasone will be concurrently administered with SCH 619734 before initiation of chemotherapy on Day 1. Subjects will record nausea and vomiting in the SPNV Subject Diary through Day 6. The quality of life assessment as measured by the Functional Living Index-Emesis Questionnaire (FLIE) will be used to measure the effect of chemotherapy-induced nausea and vomiting (CINV) on daily life. Blood samples for SCH 619734 pharmacokinetic assessments will be collected. The study is to be conducted in conformance with Good Clinical Practice.
NCT00506545 ↗ Study of the Efficacy and Safety of SCH 619734 in Subjects With Chronic Cough From an Unknown Cause (Study P04888) Completed Merck Sharp & Dohme Corp. Phase 2 2007-01-01 This is a randomized, double-blind, placebo-controlled, crossover, single center study of SCH 619734 in subjects with chronic cough from an unknown cause. Subjects will be randomized to receive SCH 619734 or placebo for 7 days with 7 days' follow-up. After a 6 week washout period, subjects will be crossed over to the other treatment. The primary objective is to evaluate the effectiveness of SCH 619734 in reducing cough reflex sensitivity as determined by a challenge with capsaicin, an agent that induces cough.
NCT00539721 ↗ A Randomized Controlled Study of Rolapitant for the Prevention of Nausea and Vomiting Following Surgery (Study P04937AM1)(COMPLETED) Completed Merck Sharp & Dohme Corp. Phase 2 2007-10-01 This is a multicenter, randomized, controlled study in women who are having elective open abdominal surgery with general anesthesia and who are expected to need patient-controlled analgesia (PCA) after surgery. The primary objective is to assess the effect of rolapitant in the prevention of postoperative nausea and vomiting as measured by the prevention of vomiting in the first 24 hours after surgery. Participation in the study may last up to 3 months. The total duration of the study will be approximately 36 weeks.
NCT01499849 ↗ Ph3 Safety/Efficacy Study of Rolapitant for the Prevention of CINV in Subjects Receiving Highly Emetogenic Chemotherapy Completed Tesaro, Inc. Phase 3 2012-02-01 This is a Phase 3, multicenter, randomized, parallel-group, double-blind, active-controlled study of rolapitant in subjects receiving HEC. Rolapitant or placebo will be administered prior to initiation of chemotherapy on Day 1 with granisetron and dexamethasone. Subjects will record all events of emesis and use of rescue medication for established nausea and/or vomiting, and will indicate the severity of nausea they experienced in each of the previous 24 hours in the Nausea and Vomiting (NV) Subject Diary prior to HEC administration through Day 6 of Cycle 1. Health-related quality of life will be measured by the FLIE Questionnaire on Day 6 of Cycle 1. Safety and tolerability will be assessed by clinical review of adverse events (AEs), physical examinations, electrocardiograms (ECGs), and safety laboratory values. All subjects are expected to complete Cycle 1 and will have the option of participating in up to five additional cycles.
NCT01500213 ↗ Ph3 Safety/Efficacy Study of Rolapitant for the Prevention of CINV in Subjects Receiving Highly Emetogenic Chemotherapy Completed Tesaro, Inc. Phase 3 2012-02-01 This is a Phase 3, multicenter, randomized, parallel-group, double-blind, active-controlled study of rolapitant in subjects receiving HEC. Rolapitant or placebo will be administered 1-2 hours prior to initiation of chemotherapy on Day 1 with granisetron and dexamethasone. Subjects will record all events of emesis and use of rescue medication for established nausea and/or vomiting, and will indicate the severity of nausea they experienced in each of the previous 24 hours in the Nausea and Vomiting (NV) Subject Diary prior to HEC administration through Day 6 of Cycle 1. Health-related quality of life will be measured by the FLIE Questionnaire on Day 6 of Cycle 1. Safety and tolerability will be assessed by clinical review of adverse events (AEs), physical examinations, electrocardiograms (ECGs), and safety laboratory values. All subjects are expected to complete Cycle 1 and will have the option of participating in up to five additional cycles.
>Trial ID >Title >Status >Phase >Start Date >Summary

Clinical Trial Conditions for Rolapitant Hydrochloride

Condition Name

Condition Name for Rolapitant Hydrochloride
Intervention Trials
Chemotherapy-induced Nausea and Vomiting 7
Nausea 1
Non Small Cell Lung Cancer 1
Postoperative Nausea and Vomiting 1
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Condition MeSH

Condition MeSH for Rolapitant Hydrochloride
Intervention Trials
Vomiting 12
Nausea 8
Carcinoma, Non-Small-Cell Lung 1
Neoplasms, Germ Cell and Embryonal 1
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Clinical Trial Locations for Rolapitant Hydrochloride

Trials by Country

Trials by Country for Rolapitant Hydrochloride
Location Trials
United States 9
Turkey 1
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Trials by US State

Trials by US State for Rolapitant Hydrochloride
Location Trials
Maryland 3
Massachusetts 3
North Carolina 1
Texas 1
New York 1
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Clinical Trial Progress for Rolapitant Hydrochloride

Clinical Trial Phase

Clinical Trial Phase for Rolapitant Hydrochloride
Clinical Trial Phase Trials
Phase 3 4
Phase 2 8
Phase 1 3
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Clinical Trial Status

Clinical Trial Status for Rolapitant Hydrochloride
Clinical Trial Phase Trials
Completed 9
Recruiting 3
Terminated 1
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Clinical Trial Sponsors for Rolapitant Hydrochloride

Sponsor Name

Sponsor Name for Rolapitant Hydrochloride
Sponsor Trials
Tesaro, Inc. 9
ECONiX Araştırma Analiz ve Danışmanlık A.Ş. 2
Merck Sharp & Dohme Corp. 2
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Sponsor Type

Sponsor Type for Rolapitant Hydrochloride
Sponsor Trials
Industry 14
Other 10
NIH 1
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Rolapitant Hydrochloride: Clinical Trials, Market Analysis, and Projections

Introduction to Rolapitant Hydrochloride

Rolapitant hydrochloride, marketed under the brand name Varubi™, is a selective and competitive neurokinin 1 (NK-1) receptor antagonist. It is primarily used for the prevention of chemotherapy-induced nausea and vomiting (CINV), particularly the delayed phase that occurs more than 24 hours after chemotherapy administration[1][5].

Clinical Trials and Approval

The FDA approved rolapitant hydrochloride on September 2, 2015, based on three phase III clinical trials. These randomized, double-blind, controlled trials were conducted by a research team that included members of the Multinational Association of Supportive Care in Cancer (MASCC). The trials demonstrated the safety and efficacy of rolapitant in reducing vomiting and the use of rescue antiemetic drugs. Patients treated with rolapitant also reported fewer episodes of nausea that interfered with their daily lives[1].

Key Findings from Clinical Trials

  • Efficacy: Rolapitant significantly reduced the incidence of delayed-phase CINV.
  • Safety: The drug was well-tolerated, with no major safety concerns identified in the trials.
  • Pharmacokinetics: Rolapitant has a long elimination half-life of approximately 7 days, allowing for a single dose to be effective over a prolonged period[1][3].

Mechanism of Action

Rolapitant works by blocking the interaction between Substance P and the NK-1 receptor in the gut and central nervous system. This mechanism prevents the late-phase CINV that typically occurs after chemotherapy. Unlike other NK-1 receptor antagonists, rolapitant does not inhibit the Cytochrome P450 enzyme CYP3A4, which reduces the risk of drug interactions[5].

Market Analysis

Current Market Size and Share

As of 2021, the global market for CINV existing and pipeline drugs was estimated to be worth approximately $1.9 billion. Rolapitant held a significant share of this market, accounting for roughly 61% of the worldwide CINV existing and pipeline drugs industry[2].

Market Projections

The global CINV market is expected to grow at a Compound Annual Growth Rate (CAGR) of 5.8% from 2022 to 2031, reaching an estimated value of $3.2 billion by the end of 2031. This growth is driven by several factors:

  • Increasing Cancer Incidence: The rise in cancer cases globally is leading to more patients undergoing chemotherapy, thereby increasing the demand for CINV medications.
  • Regional Growth: North America is expected to maintain its dominance in the market, growing at a CAGR of more than 7%. The Asia Pacific region is also anticipated to grow significantly, driven by increasing adoption of Western treatments and rising healthcare facilities in countries like India and China[2].

Regional Analysis

  • North America: This region was the largest market for CINV drugs in 2021 and is expected to continue its dominance.
  • Europe: Europe was the second-largest market in 2021, with the introduction of new CINV pipeline drugs expected to drive growth.
  • Asia Pacific: This region is experiencing rapid growth due to increased cancer prevalence and expanding healthcare facilities[2].

Competitive Landscape

The CINV market is competitive, with several drugs available, including rolapitant, SUSTOL (APF-530), Aloxi, and Emend. However, rolapitant's long-acting nature and lack of inhibition of CYP3A4 make it a preferred choice among physicians. The approval of pipeline drugs, such as SUSTOL, is also expected to drive market growth[2].

Pharmacokinetics and Metabolism

  • Absorption: Peak plasma concentrations of rolapitant are achieved in about 4 hours after administration.
  • Volume of Distribution: Rolapitant has a large volume of distribution of approximately 460 L.
  • Protein Binding: The drug is 99.8% bound to human plasma protein.
  • Metabolism: Rolapitant is metabolized primarily by the Cytochrome P450 enzyme CYP3A4 to its major active metabolite M19.
  • Route of Elimination: The major route of excretion is via the hepatic/biliary route (73%), followed by urine (14%)[3][5].

Safety and Tolerability

Rolapitant has been shown to be well-tolerated in clinical trials. However, there are considerations for patients with severe hepatic or renal impairment, as the drug's long half-life could potentially lead to accumulation and toxicity in these populations. No significant dose adjustments are necessary for patients with mild to moderate hepatic or renal impairment[3].

Pediatric and Future Studies

There are ongoing plans for pediatric studies of rolapitant, including a Phase 3, multicenter, randomized, double-blind, placebo-controlled study to evaluate the safety, efficacy, and pharmacokinetics of rolapitant in pediatric patients aged 0-17 years. Additional studies are planned to assess drug interactions and toxicology in juvenile rats[4].

Key Takeaways

  • Clinical Efficacy: Rolapitant is highly effective in preventing delayed-phase CINV.
  • Market Dominance: Rolapitant holds a significant share of the global CINV market.
  • Growth Projections: The CINV market is expected to grow significantly, driven by increasing cancer incidence and regional expansion.
  • Pharmacokinetics: Rolapitant has a favorable pharmacokinetic profile with a long half-life and high bioavailability.
  • Safety: The drug is generally well-tolerated but requires caution in patients with severe hepatic or renal impairment.

FAQs

What is rolapitant hydrochloride used for?

Rolapitant hydrochloride is used for the prevention of chemotherapy-induced nausea and vomiting (CINV), particularly the delayed phase.

When was rolapitant hydrochloride approved by the FDA?

Rolapitant hydrochloride was approved by the FDA on September 2, 2015.

What is the mechanism of action of rolapitant hydrochloride?

Rolapitant hydrochloride works by blocking the interaction between Substance P and the NK-1 receptor in the gut and central nervous system.

What is the expected growth rate of the CINV market?

The global CINV market is expected to grow at a CAGR of 5.8% from 2022 to 2031.

Which region dominates the CINV market?

North America dominates the CINV market and is expected to maintain its position of dominance.

Sources

  1. MASCC: FDA Approves Rolapitant for Chemotherapy-Induced Nausea and Vomiting.
  2. GlobeNewswire: CINV Existing and Pipeline Drugs Market to reach US$ 3.2 billion in 2031.
  3. FDA: 206500Orig1s000 - accessdata.fda.gov.
  4. FDA: 208399Orig1s000 - accessdata.fda.gov.
  5. DrugBank: Rolapitant: Uses, Interactions, Mechanism of Action | DrugBank Online.

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