doripenem
Trade name: doribax
Approved
Oct 12, 2007
Doripenem is a synthetic carbapenem that has broad antibacterial potency against aerobic and anaerobic gram-positive and gram-negative bacteria. Doripenem is structurally related to beta-lactam antibiotics and shares the bactericidal mode of action of other β-lactam antibiotics by targeting penicillin-binding proteins (PBPs) to inhibit the biosynthesis of the bacterial cell wall. Doripenem is resistant to hydrolysis by most β-lactamases and is resistant to inactivation by renal dehydropeptidases. Doripenem has many similarities to the other carbapenems, as well as some important differences, such as greater potency against Pseudomonas aeruginosa. It was found to be similar to comparator agents. The most common adverse effects related to doripenem therapy were headache, nausea, diarrhea, rash, and phlebitis. — NCATS
Clinical trial activity
26 trials · 15 clinical orgs · 2 marketing orgs
Earliest trial started Dec 1, 2003 (NCT00229021)
Timeline
2000s
- Jan 1, 2003
Johnson and Johnson — Earliest Phase 3 Sponsor(trial)
- Jan 1, 2007
Johnson and Johnson — Earliest Phase 2 Sponsor(trial)
- Oct 12, 2007
Johnson and Johnson — Earliest FDA Approval
- Oct 12, 2007
Shionogi — NDA Secondary Org
- Oct 12, 2007
Johnson and Johnson — NDA Organization
- Oct 12, 2007
Shionogi — Marketing Organization
- Jan 1, 2009
Earliest Phase 1 Sponsor(trial)
Indications
Studied for
- Abdomen, Acute · Phase 3
- Abdominal Abscess · Phase 3
- Abdominal Pain · Phase 3
- Appendicitis · Phase 3
- Bacteremia · Phase 2/Phase 3
- Bacterial Infections · Phase 4
- Bacterial Infections and Mycoses · Phase 3
- Cholecystitis · Phase 3
- Community-Acquired Infections · Phase 3
- Cross Infection · Phase 4
- Febrile Neutropenia · Phase 4
- Healthcare-Associated Pneumonia · Phase 2/Phase 3
- Healthy Volunteers · Phase 4
- Ileus · Phase 3
- Infections · Phase 4
- Intestinal Perforation · Phase 3
- Intraabdominal Infections · Phase 4
- Meningitis · Phase 1
- Pancreatitis · Phase 3
- Peritonitis · Phase 3
- Pneumonia · Phase 4
- Pneumonia, Bacterial · Phase 3
- Pneumonia, Ventilator-Associated · Phase 4
- Pyelonephritis · Phase 3
- Rupture · Phase 3
- Sepsis · Phase 4
- Ventilators, Mechanical · Phase 3
Mechanism of action
- Bacterial penicillin-binding proteinINHIBITOR
Bacterial penicillin-binding protein inhibitor
- D-alanyl-D-alanine carboxypeptidase DacB (dacB) ↗
- Peptidoglycan D,D-transpeptidase FtsI (ftsI) ↗
- Penicillin-binding protein 1A (mrcA) ↗
- Penicillin-binding protein 1B (mrcB) ↗
- D-alanyl-D-alanine carboxypeptidase DacA (dacA) ↗
- Peptidoglycan D,D-transpeptidase MrdA (mrdA) ↗
- D-alanyl-D-alanine carboxypeptidase DacC (dacC) ↗
Approval history
- approvedOct 12, 2007
Chemistry & pharmacology
SMILES
C[C@@H](O)[C@@H]1[C@H]2[C@@H](C)C(S[C@@H]3CN[C@H](CNS(N)(=O)=O)C3)=C(N2C1=O)C(O)=O- Mol. weight
- 420.504 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Discontinued
Oral
No
Parenteral
Yes
Topical
No
Sources
- WikipediaDoripenem ↗
- NCATSBHV525JOBH ↗
- ChEMBLCHEMBL491571 ↗
Also known as
- 2-(5-sulfamoylaminomethylpyrrolidin-3-ylthio)-6-(1-hydroxyethyl)-1-methylcarbapen-2-em-3-carboxylic acid
- doribax
- doribax
- doribax
- doribax
- doribax
- doribax
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem
- doripenem hydrate
- finibax
- finibax
- s 4661
- s-4661
- s-4661
- s-4661
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02134106 | Phase 2/Phase 3 (Phase 3) | Jan 1, 2015 | Changi General Hospital, Nanyang Technological University, National University of Singapore, Singapore General Hospital |
| NCT01599806 | Phase 3 | Oct 1, 2012 | AstraZeneca, Forest Laboratories |
| NCT01595438 | Phase 3 | Oct 1, 2012 | AstraZeneca, Forest Laboratories |
| NCT01366651 | Phase 1 | Mar 1, 2012 | Johnson and Johnson |
| NCT01517815 | N/A | Feb 1, 2012 | University of Montpellier |
| NCT01110382 | Phase 3 | Dec 1, 2010 | Johnson and Johnson |
| NCT01110408 | Phase 3 | Dec 1, 2010 | Johnson and Johnson |
| NCT01110421 | Phase 3 | Dec 1, 2010 | Johnson and Johnson |
| NCT01281462 | Phase 2 | Dec 1, 2010 | Forest Laboratories |
| NCT01467648 | Phase 4 | Oct 1, 2010 | Prince of Songkla University |
| NCT01311141 | Phase 4 | Aug 1, 2010 | University of Vienna |
| NCT01401010 | Phase 4 | Aug 1, 2010 | Michigan State University |
| NCT01027897 | Phase 4 | Apr 1, 2010 | Emory University, Johnson and Johnson |
| NCT01381848 | Phase 1 | Oct 1, 2009 | Johnson and Johnson |
| NCT00986102 | Phase 4 | Jul 1, 2009 | Johnson and Johnson |
| NCT00925392 | Phase 1 | Jun 1, 2009 | University of Illinois, University of Illinois at Chicago |
| NCT00965848 | Phase 4 | Jun 1, 2009 | Johnson and Johnson |
| NCT00589693 | Phase 3 | Apr 1, 2008 | Johnson and Johnson |
| NCT00515034 | Phase 2 | Oct 1, 2007 | Johnson and Johnson |
| NCT00502801 | Phase 2 | Aug 1, 2007 | Johnson and Johnson |
Organizations
Research & Development (15)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Johnson and Johnson | For profit | 17 | 16 | 4 | 2003 |
| Peninsula Pharmaceuticals | For profit | 6 | 0 | 1 | 2003 |
| Forest Laboratories | For profit | 3 | 1 | 2 | 2010 |
| AstraZeneca | For profit | 2 | 2 | 1 | 2012 |
| Changi General Hospital | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Emory University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| Michigan State University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| Nanyang Technological University | Academic/Hospital | 1 | 1 | 1 | 2015 |
| National University of Singapore | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Prince of Songkla University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| Singapore General Hospital | Academic/Hospital | 1 | 0 | 1 | 2015 |
| University of Illinois | Academic/Hospital | 1 | 0 | 1 | 2009 |
| University of Illinois at Chicago | Academic/Hospital | 1 | 1 | 1 | 2009 |
| University of Montpellier | Academic/Hospital | 1 | 1 | 1 | 2012 |
| University of Vienna | Academic/Hospital | 1 | 1 | 1 | 2010 |
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Johnson and Johnson | For profit | NDA | Oct 12, 2007 |
| Shionogi | For profit | NDA2 | Oct 12, 2007 |
| Shionogi | For profit | MKTG | Oct 12, 2007 |