Emend(aprepitant)
Aponvie, Cinvanti, Emend (aprepitant) is a small molecule pharmaceutical. Aprepitant was first approved as Emend on 2003-03-26. It has been approved in Europe to treat neoplasms, postoperative nausea and vomiting, and vomiting. The pharmaceutical is active against substance-P receptor.
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Commercial
Trade Name
FDA
EMA
Aponvie, Cinvanti, Emend (generic drugs available since 2012-09-24)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Aprepitant
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| CINVANTI | Heron Therapeutics | N-209296 RX | 2017-11-09 | 1 products, RLD, RS |
| APONVIE | Heron Therapeutics | N-216457 RX | 2022-09-16 | 1 products, RLD, RS |
| EMEND | Merck KGaA | N-021549 RX | 2003-03-26 | 2 products, RLD, RS |
| EMEND | Merck Sharp & Dohme | N-207865 RX | 2015-12-17 | 1 products, RLD, RS |
Show 1 discontinued
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent | Expires | Flag | FDA Information |
|---|---|---|---|
| Aprepitant, Aponvie, Heron Theraps Inc | |||
| 9561229 | 2035-09-18 | DP | U-2161, U-3440 |
| 9808465 | 2035-09-18 | U-2161, U-3440 | |
| 9974742 | 2035-09-18 | DP | |
| 9974793 | 2035-09-18 | DP | |
| 9974794 | 2035-09-18 | DP | U-2161, U-3440 |
| 10500208 | 2035-09-18 | DP | |
| 10624850 | 2035-09-18 | U-2161, U-3440 | |
| 10953018 | 2035-09-18 | U-2161, U-3440 | |
| 11173118 | 2035-09-18 | DP | |
| Aprepitant, Emend, Merck | |||
| 8258132 | 2027-09-26 | DP | U-901, U-1743, U-1916 |
Clinical
Clinical Trials
173 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Vomiting | D014839 | HP_0002013 | R11.1 | 8 | 20 | 23 | 10 | 10 | 70 |
| Nausea | D009325 | HP_0002018 | R11.0 | 2 | 12 | 6 | 6 | 5 | 31 |
| Postoperative nausea and vomiting | D020250 | EFO_0004888 | 2 | 2 | 3 | 12 | 7 | 25 | |
| Neoplasms | D009369 | C80 | 2 | 2 | 2 | 2 | 3 | 10 | |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 2 | — | 3 | 2 | 1 | 8 |
| Lymphoma | D008223 | C85.9 | — | 1 | — | 2 | 3 | 6 | |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | — | 1 | — | 1 | 3 | 5 |
| Pruritus | D011537 | HP_0000989 | L29 | — | 2 | — | 1 | 1 | 4 |
| Healthy volunteers/patients | — | 3 | — | — | 1 | — | 4 | ||
| Leukemia | D007938 | C95 | — | — | — | 2 | 2 | 4 |
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Major depressive disorder | D003865 | EFO_0003761 | F22 | — | — | 9 | — | — | 9 |
| Non-small-cell lung carcinoma | D002289 | — | 2 | 1 | — | 1 | 4 | ||
| Myeloproliferative disorders | D009196 | D47.1 | — | — | 1 | — | 2 | 3 | |
| Myeloid leukemia acute | D015470 | C92.0 | — | 2 | 1 | — | — | 3 | |
| Colorectal neoplasms | D015179 | — | 1 | 1 | — | 1 | 3 | ||
| Multiple myeloma | D009101 | C90.0 | 1 | 1 | 1 | — | — | 3 | |
| Gastrointestinal neoplasms | D005770 | C26.9 | — | — | 1 | — | 1 | 2 | |
| Female genital neoplasms | D005833 | — | — | 1 | — | — | 1 | ||
| Germ cell and embryonal neoplasms | D009373 | — | — | 1 | — | — | 1 | ||
| Liver neoplasms | D008113 | EFO_1001513 | C22.0 | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Alcoholism | D000437 | EFO_0003829 | F10.1 | — | 3 | — | — | — | 3 |
| Marijuana abuse | D002189 | EFO_0007191 | F12 | 1 | 2 | — | — | — | 3 |
| Myelodysplastic syndromes | D009190 | D46 | — | 1 | — | — | 2 | 3 | |
| Hypertension | D006973 | EFO_0000537 | I10 | — | 1 | — | — | 1 | 2 |
| Type 2 diabetes mellitus | D003924 | EFO_0001360 | E11 | — | 1 | — | — | 1 | 2 |
| Covid-19 | D000086382 | U07.1 | — | 1 | — | — | — | 1 | |
| Analgesia | D000698 | — | 1 | — | — | — | 1 | ||
| Head and neck neoplasms | D006258 | — | 1 | — | — | — | 1 | ||
| Glioblastoma | D005909 | EFO_0000515 | 1 | 1 | — | — | — | 1 | |
| Lung neoplasms | D008175 | C34.90 | — | 1 | — | — | — | 1 |
Show 10 more
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hiv infections | D015658 | EFO_0000764 | B20 | 3 | — | — | — | — | 3 |
| Opioid-related disorders | D009293 | EFO_0005611 | F11 | 2 | — | — | — | — | 2 |
| Tobacco use disorder | D014029 | F17 | 1 | — | — | — | — | 1 | |
| Non-hodgkin lymphoma | D008228 | C85.9 | 1 | — | — | — | — | 1 | |
| Heroin dependence | D006556 | EFO_0004240 | 1 | — | — | — | — | 1 | |
| Substance-related disorders | D019966 | EFO_0003890 | F13 | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Chronic obstructive pulmonary disease | D029424 | EFO_0000341 | J44.9 | — | — | — | — | 2 | 2 |
| Plasma cell neoplasms | D054219 | — | — | — | — | 2 | 2 | ||
| Cognitive dysfunction | D060825 | G31.84 | — | — | — | — | 1 | 1 | |
| Genetic polymorphism | D011110 | — | — | — | — | 1 | 1 | ||
| Brenner tumor | D001948 | — | — | — | — | 1 | 1 | ||
| Endometrioid carcinoma | D018269 | — | — | — | — | 1 | 1 | ||
| Fallopian tube neoplasms | D005185 | — | — | — | — | 1 | 1 | ||
| Cystadenocarcinoma | D003536 | — | — | — | — | 1 | 1 | ||
| Narcotic-related disorders | D000079524 | — | — | — | — | 1 | 1 | ||
| Pancreatitis | D010195 | EFO_0000278 | K85 | — | — | — | — | 1 | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | APREPITANT |
| INN | aprepitant |
| Description | Aprepitant is a morpholine-based antiemetic, which is or 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. It has a role as an antidepressant, an antiemetic, a peripheral nervous system drug, a neurokinin-1 receptor antagonist and a substance P receptor antagonist. It is a member of triazoles, a member of morpholines, a cyclic acetal and a member of (trifluoromethyl)benzenes. |
| Classification | Small molecule |
| Drug class | tachykinin (neurokinin) receptor antagonists: NK1 receptor antagonists |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | C[C@@H](O[C@H]1OCCN(Cc2n[nH]c(=O)[nH]2)[C@H]1c1ccc(F)cc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 |
Identifiers
| PDB | 6HLO |
| CAS-ID | 170729-80-3 |
| RxCUI | 358255 |
| ChEMBL ID | CHEMBL1471 |
| ChEBI ID | 499361 |
| PubChem CID | 135413536 |
| DrugBank | DB00673 |
| UNII ID | 1NF15YR6UY (ChemIDplus, GSRS) |
Target
Agency Approved
TACR1
TACR1
Organism
Homo sapiens
Gene name
TACR1
Gene synonyms
NK1R, TAC1R
NCBI Gene ID
Protein name
substance-P receptor
Protein synonyms
neurokinin receptor 1, NK-1 receptor, NK-1R, Tachykinin receptor 1, tachykinin receptor 1 (substance P receptor; neurokinin-1 receptor)
Uniprot ID
Mouse ortholog
Tacr1 (21336)
substance-P receptor (Q8BYR7)
Alternate
No data
Variants
Clinical Variant
No data
Financial
Cinvanti - HERON THERAPEUTICS, INC. /DE/
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Aponvie - HERON THERAPEUTICS, INC. /DE/
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Emend - Merck Sharp & Dohme
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Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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113,559 adverse events reported
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