Overview
Benztropine, with the chemical formula 3alpha-diphenylmethoxytropane, is a tropane-based dopamine inhibitor used for the symptomatic treatment of Parkinson's disease. It is a combination molecule between a tropane ring, similar to cocaine, and a diphenyl ether from the dialkylpiperazines determined to be a dopamine uptake inhibitor since 1970. The generation of structure-activity relationships proved that benztropine derivatives with the presence of a chlorine substituent in the para position in one of the phenyl rings produces an increased potency for dopamine uptake inhibition as well as a decreased inhibition of serotonin and norepinephrine. Benztropine was developed by USL Pharma and officially approved by the FDA on 1996.
Background
Benztropine, with the chemical formula 3alpha-diphenylmethoxytropane, is a tropane-based dopamine inhibitor used for the symptomatic treatment of Parkinson's disease. It is a combination molecule between a tropane ring, similar to cocaine, and a diphenyl ether from the dialkylpiperazines determined to be a dopamine uptake inhibitor since 1970. The generation of structure-activity relationships proved that benztropine derivatives with the presence of a chlorine substituent in the para position in one of the phenyl rings produces an increased potency for dopamine uptake inhibition as well as a decreased inhibition of serotonin and norepinephrine. Benztropine was developed by USL Pharma and officially approved by the FDA on 1996.
Indication
用于治疗帕金森病。也用于药物引起的锥体外系疾患，口服1小时起效，肌肉或静脉注射数分钟内起效，作用持续24小时。具有抗胆碱及抗组胺作用，并有轻度局部麻醉作用。
Associated Conditions
- Parkinsonism
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/01/01 | Phase 1 | Recruiting | |||
2024/01/30 | Phase 4 | Recruiting | Aarhus University Hospital | ||
2023/09/13 | N/A | ENROLLING_BY_INVITATION | |||
2023/06/02 | Phase 2 | Recruiting | |||
2022/05/19 | Phase 1 | Completed | |||
2022/04/11 | Phase 3 | Recruiting | |||
2022/03/10 | Phase 2 | UNKNOWN | Peking University Cancer Hospital & Institute | ||
2021/07/12 | Not Applicable | Completed | |||
2020/12/28 | Phase 1 | Completed | |||
2019/12/09 | Phase 2 | UNKNOWN |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Aphena Pharma Solutions - Tennessee, LLC | 43353-913 | ORAL | 0.5 mg in 1 1 | 5/21/2014 | |
| TYA Pharmaceuticals | 64725-0012 | INTRAVENOUS, INTRAMUSCULAR | 1 mg in 1 mL | 8/10/2012 | |
| Contract Pharmacy Services-PA | 67046-207 | ORAL | 1 mg in 1 1 | 12/19/2018 | |
| Par Pharmaceutical, Inc. | 0603-2439 | ORAL | 2 mg in 1 1 | 3/27/2023 | |
| Marlex Pharmaceuticals Inc | 10135-608 | ORAL | 2 mg in 1 1 | 5/17/2019 | |
| Marlex Pharmaceuticals Inc | 10135-607 | ORAL | 1 mg in 1 1 | 5/17/2019 | |
| Bryant Ranch Prepack | 63629-2135 | ORAL | 2 mg in 1 1 | 1/11/2024 | |
| Bayshore Pharmaceuticals LLC (NJ) | 76385-103 | ORAL | 0.5 mg in 1 1 | 3/14/2019 | |
| Cipla USA Inc. | 69097-827 | ORAL | 1 mg in 1 1 | 12/11/2018 | |
| Major Pharmaceuticals | 0904-6789 | ORAL | 2 mg in 1 1 | 8/8/2019 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| BENZATROPINE PHEBRA SOLUTION FOR INJECTION 2 MG/2 ML | SIN16222P | INJECTION, SOLUTION | 2.0 mg/2ml | 6/3/2021 | |
| APO-BENZTROPINE TABLET 2 mg | SIN05894P | TABLET | 2 mg | 5/22/1991 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Benzatropine Hydrobromide Tablets | 国药准字H11021858 | 化学药品 | 片剂 | 11/2/2020 |
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 |
|---|---|---|---|---|---|
| Benzatropine Injection | 320907 | Medicine | A | 7/26/2019 | |
| BENZTROP benztropine mesilate 2mg tablet bottle | 83130 | Medicine | A | 7/15/2002 | |
| BENZATROPINE INJECTION benzatropine mesilate 2mg in 2 mL, vial | 276242 | Medicine | A | 7/18/2017 |