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1. Cns 7056
2. Methyl 3-(8-bromo-1-methyl-6-(2-pyridinyl)-4h-imidazo(1,2-a)(1,4)benzodiazepin-4-yl)propanoate
3. Ono 2745
4. Ono-2745
5. Ono2745
1. 308242-62-8
2. Cns 7056
3. Cns-7056
4. Ono-2745
5. 7v4a8u16mb
6. 308242-62-8 (freee Base)
7. 4h-imidazo(1,2-a)(1,4)benzodiazepine-4-propanoic Acid, 8-bromo-1-methyl-6-(2-pyridinyl)-, Methyl Ester, (4s)-
8. Methyl (s)-3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4h-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate
9. Remimazolam [inn]
10. Unii-7v4a8u16mb
11. Remimazolam [mi]
12. Remimazolam (usan/inn)
13. Remimazolam [usan:inn]
14. Remimazolam [usan]
15. Remimazolam [who-dd]
16. Schembl846435
17. Chembl4297526
18. Dtxsid20953024
19. Ono2745
20. Amy15524
21. Ex-a5536
22. Ono 2745
23. Who 9232
24. Zinc3927450
25. Akos025213215
26. Db12404
27. Hy-14867
28. 4523b
29. Cs-0003605
30. D11788
31. 4h-imidazol(1,2-a)(1,4)benzodiazepine-4-propionic Acid, (s)-
32. (s)-methyl 3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4h-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate
33. Methyl 3-((4s)-8-bromo-1-methyl-6-(pyridin-2-yl)-4h-imidazo(1,2-a)(1,4)benzodiazepin-4-yl)propanoate
34. Methyl 3-[(4s)-8-bromo-1-methyl-6-(2-pyridyl)-4h-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate
35. Methyl 3-[(4s)-8-bromo-1-methyl-6-pyridin-2-yl-4h-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate
36. Methyl 3-[8-bromo-1-methyl-6-(pyridin-2-yl)-4h-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate
Molecular Weight | 439.3 g/mol |
---|---|
Molecular Formula | C21H19BrN4O2 |
XLogP3 | 3.4 |
Hydrogen Bond Donor Count | 0 |
Hydrogen Bond Acceptor Count | 5 |
Rotatable Bond Count | 5 |
Exact Mass | 438.06914 g/mol |
Monoisotopic Mass | 438.06914 g/mol |
Topological Polar Surface Area | 69.4 Ų |
Heavy Atom Count | 28 |
Formal Charge | 0 |
Complexity | 601 |
Isotope Atom Count | 0 |
Defined Atom Stereocenter Count | 1 |
Undefined Atom Stereocenter Count | 0 |
Defined Bond Stereocenter Count | 0 |
Undefined Bond Stereocenter Count | 0 |
Covalently Bonded Unit Count | 1 |
Remimazolam is indicated for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less.
FDA Label
Remimazolam is indicated in adults for procedural sedation.
Remimazolam modulates the effects of GABA(A) receptors in order to enhance the effects of GABA. It is considered an "ultra short-acting" benzodiazepine that achieves peak sedation within 3 to 3.5 minutes following intravenous administration, a property that makes it desirable for use during short procedures. Hepatic impairment can result in elevated serum levels of remimazolam - patients with severe hepatic impairment should be carefully titrated to effect. As of its approval date, remimazolam has not received a scheduling action by the DEA under the Controlled Substances Act. As benzodiazepines as a class have been implicated in the development of drug dependence and have a known potential for abuse, remimazolam should be used with caution in patients with a history of drug dependence or abuse.
N05CD
N - Nervous system
N05 - Psycholeptics
N05C - Hypnotics and sedatives
N05CD - Benzodiazepine derivatives
N05CD14 - Remimazolam
Absorption
The Cmax and AUC0-inf following intravenous administration of 0.01 to 0.5 mg/kg were 189 to 6,960 ng/mL and 12.1 to 452 ngh/mL, respectively, and appear to be relatively dose proportional. The Tmax of the inactive CNS7054 metabolite is approximately 20-30 minutes and its AUC0-inf ranges from 231 to 7,090 ngh/mL.
Route of Elimination
In patients undergoing colonoscopy, approximately 0.003% of the administered dose is excreted in the urine as unchanged parent drug and 50-60% is excreted in the urine as CNS7054. In healthy subjects, >80% of the administered dose is excreted in the urine as CNS7054.
Volume of Distribution
The volume of distribution is approximately 0.76 - 0.98 L/kg.
Clearance
The clearance of remimazolam is approximately 24 - 75 L/h and is independent of body weight.
Remimazolam does not appear to undergo biotransformation via hepatic cytochrome P450 enzymes, nor does it induce or inhibit these enzymes. Its primary route of metabolism is hydrolysis via hepatic carboxylesterase-1 (CES1) to yield the inactive CNS7054 metabolite, which then undergoes glucuronidation and hydroxylation prior to elimination. CNS7054 possesses a 300-fold lesser affinity for GABA(A) receptors as compared to the parent drug.
Following intravenous administration, the distribution half-life is of remimazolam is 0.5 - 2 minutes and the terminal elimination half-life is 37 - 53 minutes. Half-life is increased in patients with hepatic impairment necessitating careful dose titration in this population. The half-life of remimazolam's major inactive metabolite, CNS7054, is 2.4 - 3.8 hours.
Like other benzodiazepines, remimazolam exerts its therapeutic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA(A) receptors, the main inhibitory neurotransmitter receptors in the mammalian brain. GABA(A) receptors are a component of GABA-gated ionotropic chloride channels that produce inhibitory postsynaptic potentials - following activation by GABA, the channel undergoes a conformational change that allows the passage of chloride ions through the channel. The inhibitory potentials produced by GABA neurotransmission play an integral role in the suppression and control of epileptiform nerve firing such as that seen in epilepsy, which makes the GABA system a desirable target in the treatment of epilepsy. Benzodiazepines are positive allosteric modulators of GABA(A) function. They bind to the interface between alpha () and gamma () subunits on the receptor, commonly referred to as the benzodiazepine binding site, and modulate the receptor such that its inhibitory response to GABA binding is dramatically increased.
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 36332
Submission : 2021-10-07
Status : Active
Type : II
GDUFA
DMF Review : N/A
Rev. Date :
Pay. Date :
DMF Number : 32748
Submission : 2019-03-15
Status : Active
Type : II
GDUFA
DMF Review : Complete
Rev. Date : 2024-08-29
Pay. Date : 2024-05-01
DMF Number : 39813
Submission : 2024-05-30
Status : Active
Type : II
Registrant Name : Samoh Pharmaceutical Co., Ltd.
Registration Date : 2021-01-07
Registration Number : Su0106-1-ND
Manufacturer Name : Cambrex, Karlskoga AB
Manufacturer Address : Bjorkborn Industriomrade Karlskoga, 691 85 Sweden
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Details:
BYFAVO is the second Acacia Pharma product approved and launched in the US in the last year and extends its portfolio of new products targeting unmet needs in anesthesia.
Lead Product(s): Remimazolam Besylate
Therapeutic Area: Neurology Brand Name: Byfavo
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable January 28, 2021
Lead Product(s) : Remimazolam Besylate
Therapeutic Area : Neurology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : BYFAVO is the second Acacia Pharma product approved and launched in the US in the last year and extends its portfolio of new products targeting unmet needs in anesthesia.
Brand Name : Byfavo
Molecule Type : Small molecule
Upfront Cash : Not Applicable
January 28, 2021
Details:
Under the Investment Agreement, Cosmo would have become eligible to receive a €5 million payment from the Company payable in new ordinary shares in the Company conditional upon the first commercial sale of the BYFAVO™ product in the United States.
Lead Product(s): Remimazolam Besylate
Therapeutic Area: Neurology Brand Name: Byfavo
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Acacia Pharma
Deal Size: $45.0 million Upfront Cash: Undisclosed
Deal Type: Agreement December 15, 2020
Lead Product(s) : Remimazolam Besylate
Therapeutic Area : Neurology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Acacia Pharma
Deal Size : $45.0 million
Deal Type : Agreement
Details : Under the Investment Agreement, Cosmo would have become eligible to receive a €5 million payment from the Company payable in new ordinary shares in the Company conditional upon the first commercial sale of the BYFAVO™ product in the United States.
Brand Name : Byfavo
Molecule Type : Small molecule
Upfront Cash : Undisclosed
December 15, 2020
Details:
US DEA has designated its procedural sedative BYFAVO™ (remimazolam injection) as a Schedule IV medicine. This designation is the schedule for drugs with a low potential for abuse and low risk of dependence and is consistent with that granted to many other benzodiazepine drugs.
Lead Product(s): Remimazolam Besylate
Therapeutic Area: Neurology Brand Name: Byfavo
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable October 06, 2020
Lead Product(s) : Remimazolam Besylate
Therapeutic Area : Neurology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Acacia Pharma Announces BYFAVO its Newly Approved Product for Procedural Sedation
Details : US DEA has designated its procedural sedative BYFAVO™ (remimazolam injection) as a Schedule IV medicine. This designation is the schedule for drugs with a low potential for abuse and low risk of dependence and is consistent with that granted to many ot...
Brand Name : Byfavo
Molecule Type : Small molecule
Upfront Cash : Not Applicable
October 06, 2020
Details:
Acacia Pharma has been assigned the US license to BYFAVO™ (remimazolam) for injection by Cosmo Pharmaceuticals NV. BYFAVO for injection is a very rapid onset/offset intravenous benzodiazepine sedative for use during invasive medical procedures lasting 30 minutes or less.
Lead Product(s): Remimazolam Besylate
Therapeutic Area: Neurology Brand Name: Byfavo
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Acacia Pharma
Deal Size: Undisclosed Upfront Cash: Undisclosed
Deal Type: Licensing Agreement July 15, 2020
Lead Product(s) : Remimazolam Besylate
Therapeutic Area : Neurology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Acacia Pharma
Deal Size : Undisclosed
Deal Type : Licensing Agreement
Acacia Pharma Assigned US License for BYFAVO™ (remimazolam) by Cosmo Pharmaceuticals NV
Details : Acacia Pharma has been assigned the US license to BYFAVO™ (remimazolam) for injection by Cosmo Pharmaceuticals NV. BYFAVO for injection is a very rapid onset/offset intravenous benzodiazepine sedative for use during invasive medical procedures lasting ...
Brand Name : Byfavo
Molecule Type : Small molecule
Upfront Cash : Undisclosed
July 15, 2020
Details:
The US Food and Drug Administration (FDA) has approved BYFAVO™ (remimazolam injection) for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less.
Lead Product(s): Remimazolam Besylate
Therapeutic Area: Neurology Brand Name: Byfavo
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable July 02, 2020
Lead Product(s) : Remimazolam Besylate
Therapeutic Area : Neurology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Cosmo Pharmaceuticals Announces US FDA Approval of BYFAVO™ (remimazolam injection)
Details : The US Food and Drug Administration (FDA) has approved BYFAVO™ (remimazolam injection) for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less.
Brand Name : Byfavo
Molecule Type : Small molecule
Upfront Cash : Not Applicable
July 02, 2020
Details:
Acacia Pharma will be responsible for the marketing and distribution of ByFavo in the US in the context of its equity-for-product strategy.
Lead Product(s): Remimazolam Besylate
Therapeutic Area: Neurology Brand Name: Undisclosed
Study Phase: Phase IIIProduct Type: Small molecule
Sponsor: Cosmo Pharmaceuticals
Deal Size: $143.2 million Upfront Cash: $11.1 million
Deal Type: Licensing Agreement January 09, 2020
Lead Product(s) : Remimazolam Besylate
Therapeutic Area : Neurology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Cosmo Pharmaceuticals
Deal Size : $143.2 million
Deal Type : Licensing Agreement
Issue of Equity on Share Subscription and Licensing agreement With Cosmo Pharmaceuticals
Details : Acacia Pharma will be responsible for the marketing and distribution of ByFavo in the US in the context of its equity-for-product strategy.
Brand Name : Undisclosed
Molecule Type : Small molecule
Upfront Cash : $11.1 million
January 09, 2020
Methyl 3-((3S)-7-bromo-2-((2-hydroxypropyl)amino)-...
CAS Number : 308243-54-1
End Use API : Remimazolam Besylate
About The Company : Cohance Lifesciences is a leading CDMO and API platform, offering products and services across all phases of a molecule’s lifecycle from development to commer...
(3S)-(7-BroMo-2-oxo-5-pyridin-2-yl-2,3-dihydro-1H-...
CAS Number : 308242-23-1
End Use API : Remimazolam Besylate
About The Company : We are one of the well-known manufacturers of key APIs & intermediates in China, with 20 years of experience & presence in 20+ countries. At Boyuan, we are comm...
Regulatory Info : RX
Registration Country : USA
Brand Name : BYFAVO
Dosage Form : POWDER;INTRAVENOUS
Dosage Strength : EQ 20MG BASE/VIAL
Packaging :
Approval Date : 2020-10-06
Application Number : 212295
Regulatory Info : RX
Registration Country : USA
RLD : Yes
TE Code :
Brand Name : BYFAVO
Dosage Form : POWDER;INTRAVENOUS
Dosage Strength : EQ 20MG BASE/VIAL
Approval Date : 2020-10-06
Application Number : 212295
RX/OTC/DISCN : RX
RLD : Yes
TE Code :
Market Place
Patents & EXCLUSIVITIES
Exclusivity Code : NCE
Exclusivity Expiration Date : 2025-10-06
Application Number : 212295
Product Number : 1
Exclusivity Details :
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