dalfopristin
Trade name: Synercid
Approved
Sep 21, 1999
Dalfopristin is a pristinamycin-like component of anti-bacterial drug called Synercid which also containes quinupristin (quinupristin:dalfopristin ratio is 30:70 (w/w)). The drug was approved by FDA and used for the treatment of skin diseases caused by Staphylococcus aureus or Streptococcus pyogenes. Dalfopristin binds to the RNA of the 50S ribosomal subunit and thus inhibits the late phase of protein synthesis. — NCATS
Clinical trial activity
1 trials · 3 clinical orgs · 2 marketing orgs
Earliest trial started Jun 1, 2000 (NCT00240747)
Timeline
1990s
- Sep 21, 1999
Earliest FDA Approval
- Sep 21, 1999
King Pharmaceuticals — NDA Secondary Org
2000s
- Jan 1, 2000
Earliest Phase 3 Sponsor(trial)
Indications
Approved for
Studied for
Mechanism of action
- Bacterial 70S ribosomeINHIBITOR
Bacterial 70S ribosome inhibitor
23S RRNA
- 30S ribosomal protein S2 (rpsB) ↗
- 50S ribosomal protein L4 (rplD) ↗
- 30S ribosomal protein S15 (rpsO) ↗
- 30S ribosomal protein S16 (rpsP) ↗
- 30S ribosomal protein S17 (rpsQ) ↗
- 30S ribosomal protein S18 (rpsR) ↗
- 30S ribosomal protein S19 (rpsS) ↗
- 30S ribosomal protein S20 (rpsT) ↗
- 30S ribosomal protein S21 (rpsU) ↗
- 30S ribosomal protein S3 (rpsC) ↗
- 30S ribosomal protein S4 (rpsD) ↗
- 30S ribosomal protein S5 (rpsE) ↗
- 30S ribosomal protein S6 (rpsF) ↗
- 30S ribosomal protein S7 (rpsG) ↗
- 30S ribosomal protein S8 (rpsH) ↗
- 30S ribosomal protein S9 (rpsI) ↗
- 50S ribosomal protein L35 (rpmI) ↗
- 50S ribosomal protein L36 2 (ykgO) ↗
- 50S ribosomal protein L36 (rpmJ) ↗
- 50S ribosomal protein L3 (rplC) ↗
- 50S ribosomal protein L5 (rplE) ↗
- 50S ribosomal protein L6 (rplF) ↗
- 50S ribosomal protein L7/L12 (rplL) ↗
- 30S ribosomal protein S1 (rpsA) ↗
- 30S ribosomal protein S10 (rpsJ) ↗
- 30S ribosomal protein S11 (rpsK) ↗
- 30S ribosomal protein S12 (rpsL) ↗
- 30S ribosomal protein S13 (rpsM) ↗
- 30S ribosomal protein S14 (rpsN) ↗
- 50S ribosomal protein L10 (rplJ) ↗
- 50S ribosomal protein L11 (rplK) ↗
- 50S ribosomal protein L13 (rplM) ↗
- 50S ribosomal protein L14 (rplN) ↗
- 50S ribosomal protein L15 (rplO) ↗
- 50S ribosomal protein L16 (rplP) ↗
- 50S ribosomal protein L17 (rplQ) ↗
- 50S ribosomal protein L18 (rplR) ↗
- 50S ribosomal protein L19 (rplS) ↗
- 50S ribosomal protein L1 (rplA) ↗
- 50S ribosomal protein L20 (rplT) ↗
- 50S ribosomal protein L21 (rplU) ↗
- 50S ribosomal protein L22 (rplV) ↗
- 50S ribosomal protein L23 (rplW) ↗
- 50S ribosomal protein L24 (rplX) ↗
- 50S ribosomal protein L25 (rplY) ↗
- 50S ribosomal protein L27 (rpmA) ↗
- 50S ribosomal protein L28 (rpmB) ↗
- 50S ribosomal protein L29 (rpmC) ↗
- 50S ribosomal protein L2 (rplB) ↗
- 50S ribosomal protein L30 (rpmD) ↗
- 50S ribosomal protein L31 type B (ykgM) ↗
- 50S ribosomal protein L31 (rpmE) ↗
- 50S ribosomal protein L32 (rpmF) ↗
- 50S ribosomal protein L33 (rpmG) ↗
- 50S ribosomal protein L34 (rpmH) ↗
Combination products
synerci
with quinupristin
Also known as dalfopristin/quinupristin
Approval history
- approvedPriority reviewAcceleratedSep 21, 1999
Chemistry & pharmacology
SMILES
CCN(CC)CCS(=O)(=O)[C@@H]1CCN2[C@H]1C(=O)O[C@H](C(C)C)[C@H](C)\C=C\C(=O)NC\C=C\C(C)=C\[C@@H](O)CC(=O)CC3=NC(=CO3)C2=O- Mol. weight
- 690.847 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Discontinued
Oral
No
Parenteral
Yes
Topical
No
Sources
- WikipediaDalfopristin ↗
- NCATSR9M4FJE48E ↗
- ChEMBLCHEMBL1200937 ↗
Also known as
- 26-(2-diethylaminoethyl)sulfonylpristamycin iib
- dalfopristin
- dalfopristin
- dalfopristin
- dalfopristin
- dalfopristin
- dalfopristin
- dalfopristin
- dalfopristin
- dalfopristin
- dalfopristina
- dalfopristina
- dalfopristine
- dalfopristine
- dalfopristin mesilate
- dalfopristin mesilate
- dalfopristin mesilate
- dalfopristin mesilate
- dalfopristin mesilate
- dalfopristin mesylate
- dalfopristinum
- dalfopristinum
- rp 54476
- rp-54476
- rp-54476
- rp-54476
- rp-54476
- synercid
- synercid
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00240747 | Phase 3 | Jun 1, 2000 | Aventis, Pfizer, Yale University |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Aventis | For profit | 1 | 0 | 1 | 2000 |
| Pfizer | For profit | 1 | 1 | 1 | 2000 |
| Yale University | Academic/Hospital | 1 | 0 | 1 | 2000 |
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Aventis | For profit | NDA | — |
| King Pharmaceuticals | For profit | NDA2 | Sep 21, 1999 |