Overview
Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).
Indication
For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents).
Associated Conditions
- Chemotherapy-Induced Nausea and Vomiting
- Post Operative Nausea and Vomiting (PONV)
- Acute delayed Nausea caused by highly emetogenic cancer chemotherapy
Research Report
Aprepitant (DB00673): A Comprehensive Monograph on a First-in-Class Neurokinin-1 Receptor Antagonist
1.0 Executive Summary
Aprepitant represents a landmark achievement in supportive care, establishing a new therapeutic class as the first-in-class, selective, high-affinity neurokinin-1 (NK-1) receptor antagonist. Its development was predicated on a sophisticated understanding of the pathophysiology of emesis, specifically targeting the substance P-mediated neural pathways responsible for delayed-phase nausea and vomiting. This mechanism distinguishes it from and makes it complementary to established antiemetics like 5-hydroxytryptamine-3 (5-HT3) receptor antagonists and corticosteroids. Clinically, Aprepitant has fundamentally altered treatment paradigms for the prevention of both Chemotherapy-Induced Nausea and Vomiting (CINV) and Postoperative Nausea and Vomiting (PONV). When integrated into a triple-therapy regimen, it has demonstrated superior efficacy over standard dual-therapy, particularly in controlling the debilitating delayed symptoms of CINV associated with highly and moderately emetogenic chemotherapies.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/04/17 | Phase 3 | Completed | |||
2024/11/20 | Phase 4 | Completed | The First Affiliated Hospital of Zhengzhou University | ||
2024/08/09 | Phase 3 | Not yet recruiting | |||
2024/06/17 | Phase 2 | Recruiting | University Hospital, Rouen | ||
2024/04/10 | Phase 2 | Recruiting | |||
2023/10/12 | Not Applicable | Recruiting | Hubei Cancer Hospital | ||
2023/08/23 | Phase 4 | Recruiting | Sichuan Cancer Hospital and Research Institute | ||
2023/05/03 | Phase 4 | Not yet recruiting | Second Affiliated Hospital, School of Medicine, Zhejiang University | ||
2023/03/16 | Phase 4 | Active, not recruiting | Hospital General Tlahuac | ||
2023/02/03 | Phase 3 | Not yet recruiting | Guangxi Medical University |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Merck Sharp & Dohme LLC | 0006-3066 | ORAL | 125 mg in 1 1 | 5/6/2022 | |
| Torrent Pharmaceuticals Limited | 13668-593 | ORAL | 125 mg in 1 1 | 3/14/2023 | |
| Merck Sharp & Dohme LLC | 0006-0461 | ORAL | 80 mg in 1 1 | 5/6/2022 | |
| Heron Therapeutics, Inc. | 47426-401 | INTRAVENOUS | 32 mg in 4.4 mL | 3/13/2024 | |
| Sandoz Inc | 0781-2322 | ORAL | 80 mg in 1 1 | 12/24/2020 | |
| Heron Therapeutics, Inc. | 47426-201 | INTRAVENOUS | 130 mg in 18 mL | 3/13/2024 | |
| Glenmark Pharmaceuticals Inc., USA | 68462-585 | ORAL | 125 mg in 1 1 | 1/28/2020 | |
| Merck Sharp & Dohme LLC | 0006-0464 | ORAL | 40 mg in 1 1 | 5/6/2022 | |
| Merck Sharp & Dohme LLC | 0006-0462 | ORAL | 125 mg in 1 1 | 5/6/2022 | |
| Sandoz Inc | 0781-2321 | ORAL | 40 mg in 1 1 | 12/24/2020 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 11/11/2003 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| INAPITANT TRI-PACK CAPSULE | SIN16363P | CAPSULE | 125.00mg | 11/5/2021 | |
| EMEND TRI-PACK CAPSULE | SIN12371P | CAPSULE | 80 mg | 7/26/2003 | |
| EMEND CAPSULE 80 mg | SIN12369P | CAPSULE | 80 mg | 7/26/2003 | |
| INAPITANT TRI-PACK CAPSULE | SIN16363P | CAPSULE | 80.00mg | 11/5/2021 | |
| EMEND TRI-PACK CAPSULE | SIN12371P | CAPSULE | 125 mg | 7/26/2003 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| APREPITANT-RJIC aprepitant 80 mg & 125 mg tri-pack capsule blister pack | 422872 | Medicine | A | 3/21/2024 | |
| APREPITANT LUPIN aprepitant 40 mg capsule blister pack | 310215 | Medicine | A | 7/3/2019 | |
| APREPITANT-RJIC aprepitant 40 mg capsule blister pack | 422870 | Medicine | A | 3/21/2024 | |
| APREPITANT ARX aprepitant 165 mg capsule blister pack | 309382 | Medicine | A | 6/11/2019 | |
| APREPITANT-RJIC aprepitant 80 mg capsule blister pack | 422871 | Medicine | A | 3/21/2024 | |
| APREPITANT-DWRN aprepitant 80 mg & 125 mg tri-pack capsule blister pack | 422812 | Medicine | A | 3/21/2024 | |
| APREPITANT LUPIN aprepitant 125 mg capsule blister pack | 310216 | Medicine | A | 7/3/2019 | |
| APREPITANT LUPIN aprepitant 80 mg capsule blister pack | 319700 | Medicine | A | 7/3/2019 | |
| APREPITANT-DWRN aprepitant 80 mg capsule blister pack | 422811 | Medicine | A | 3/21/2024 | |
| APREPITANT-DWRN aprepitant 40 mg capsule blister pack | 422810 | Medicine | A | 3/21/2024 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| EMEND | Merck Canada Inc | 02298791 | Capsule - Oral | 80 MG | 9/24/2007 |
| EMEND TRI-PACK | Merck Canada Inc | 02298813 | Kit
,
Capsule - Oral | 125 MG | 9/24/2007 |
| EMEND TRI-PACK | Merck Canada Inc | 02298813 | Kit
,
Capsule - Oral | 80 MG | 9/24/2007 |
| EMEND | Merck Canada Inc | 02298805 | Capsule - Oral | 125 MG | 9/24/2007 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| APREPITANT QILU 80 MG CAPSULAS DURAS EFG | 85689 | CÁPSULA DURA | Uso Hospitalario | Not Commercialized | |
| EMEND 125 MG POLVO PARA SUSPENSION ORAL | 103262011 | POLVO PARA SUSPENSIÓN ORAL | Uso Hospitalario | Not Commercialized | |
| ATANTO 125 MG CAPSULAS DURAS EFG/ATANTO 80 MG CAPSULAS DURAS EFG | 84704 | CÁPSULA DURA | Uso Hospitalario | Not Commercialized | |
| APREPITANT ACCORD 80 MG CAPSULAS DURAS EFG | 84277 | CÁPSULA DURA | Diagnóstico Hospitalario | Not Commercialized | |
| APREPITANT ACCORD 125 MG CAPSULAS DURAS EFG/APREPITANT ACCORD 80 MG CAPSULAS DURAS EFG | 84276 | CÁPSULA DURA | Uso Hospitalario | Commercialized | |
| APREPITANT ACCORD 125 MG CAPSULAS DURAS EFG | 84275 | CÁPSULA DURA | Uso Hospitalario | Not Commercialized | |
| ATANTO 125 MG CAPSULAS DURAS EFG | 84706 | CÁPSULA DURA | Uso Hospitalario | Not Commercialized | |
| ATANTO 80 MG CAPSULAS DURAS EFG | 84705 | CÁPSULA DURA | Diagnóstico Hospitalario | Not Commercialized | |
| APREPITANT SANDOZ 125 MG CAPSULAS DURAS EFG/APREPITANT SANDOZ 80 MG CAPSULAS DURAS EFG | Sandoz Farmaceutica S.A. | 84781 | CÁPSULA DURA | Uso Hospitalario | Commercialized |
| EMEND 80 MG CAPSULAS DURAS | 03262002 | CÁPSULA DURA | Diagnóstico Hospitalario | Not Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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