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Synopsis

Synopsis

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Chemistry

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Also known as: Vazegepant, Bms-742413, Bhv-3500, Zavegepant [usan], Odu3zaz94j, Bms-742413-01
Molecular Formula
C36H46N8O3
Molecular Weight
638.8  g/mol
InChI Key
JJVAPHYEOZSKJZ-JGCGQSQUSA-N
FDA UNII
ODU3ZAZ94J

Zavegepant HCl
Zavegepant is a highly soluble small molecule calcitonin gene related peptide (CGRP) receptor antagonist, with potential analgesic and immunomodulating activities. Upon administration, zavegepant targets, binds to and inhibits the activity of CGRP receptors located on mast cells in the brain. This may inhibit neurogenic inflammation caused by trigeminal nerve release of CGRP. In addition, by blocking the CGRP receptors located in smooth muscle cells within vessel walls, zavegepant inhibits the pathologic dilation of intracranial arteries. Zavegepant, by blocking the CGRP receptors, also suppresses the transmission of pain by inhibiting the central relay of pain signals from the trigeminal nerve to the caudal trigeminal nucleus. Altogether, this may relieve migraine. As CGRP receptors induce the release of pro-inflammatory mediators, such as interleukin-6 (IL-6), from inflammatory cells, zavegepant may prevent an IL-6-mediated inflammatory response. Zavegepant may also inhibit the CGRP-mediated induction of eosinophil migration and the stimulation of beta-integrin-mediated T cell adhesion to fibronectin at the site of inflammation, and may abrogate the CGRP-mediated polarization of the T cell response towards the pro-inflammatory state characterized by Th17 and IL-17. This may improve lung inflammation and oxygenation, prevent edema, and further lung injury. CGRP, a 37 amino-acid peptide expressed in and released from a subset of polymodal primary sensory neurons of the trigeminal ganglion and nerve fibers projecting to the airways and by pulmonary neuroendocrine cells, plays an important role in pain transmission, inflammation, and neurogenic vasodilatation. It is released upon acute lung injury and upregulation of transient receptor potential (TRP) channels.
1 2D Structure

Zavegepant HCl

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-1-oxopropan-2-yl]-4-(2-oxo-1H-quinolin-3-yl)piperidine-1-carboxamide
2.1.2 InChI
InChI=1S/C36H46N8O3/c1-24-19-25(20-28-23-37-40-33(24)28)21-32(35(46)43-17-15-42(16-18-43)29-9-11-41(2)12-10-29)39-36(47)44-13-7-26(8-14-44)30-22-27-5-3-4-6-31(27)38-34(30)45/h3-6,19-20,22-23,26,29,32H,7-18,21H2,1-2H3,(H,37,40)(H,38,45)(H,39,47)/t32-/m1/s1
2.1.3 InChI Key
JJVAPHYEOZSKJZ-JGCGQSQUSA-N
2.1.4 Canonical SMILES
CC1=CC(=CC2=C1NN=C2)CC(C(=O)N3CCN(CC3)C4CCN(CC4)C)NC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O
2.1.5 Isomeric SMILES
CC1=CC(=CC2=C1NN=C2)C[C@H](C(=O)N3CCN(CC3)C4CCN(CC4)C)NC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O
2.2 Other Identifiers
2.2.1 UNII
ODU3ZAZ94J
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Bms 742413

2. Bms-742413

3. N-(3-(7-methyl-1h-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl))-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide

2.3.2 Depositor-Supplied Synonyms

1. Vazegepant

2. Bms-742413

3. Bhv-3500

4. Zavegepant [usan]

5. Odu3zaz94j

6. Bms-742413-01

7. 1337918-83-8

8. Chembl2397415

9. N-[(2r)-3-(7-methyl-1h-indazol-5-yl)-1-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-1-oxopropan-2-yl]-4-(2-oxo-1h-quinolin-3-yl)piperidine-1-carboxamide

10. 1-piperidinecarboxamide, 4-(1,2-dihydro-2-oxo-3-quinolinyl)-n-((1r)-1-((7-methyl-1h-indazol-5-yl)methyl)-2-(4-(1-methyl-4-piperidinyl)-1-piperazinyl)-2-oxoethyl)-

11. 4-(1,2-dihydro-2-oxo-3-quinolinyl)-n-((1r)-1-((7-methyl-1h-indazol-5-yl)methyl)-2-(4-(1-methyl-4-piperidinyl)-1-piperazinyl)-2-oxoethyl)-1-piperidinecarboxamide

12. Zavegepant [inn]

13. Unii-odu3zaz94j

14. Vazegepant [who-dd]

15. Schembl107428

16. Gtpl11513

17. Ex-a6698

18. Bdbm50436107

19. Bms742413

20. Who 11512

21. Hy-134992

22. Cs-0168642

2.4 Create Date
2011-11-07
3 Chemical and Physical Properties
Molecular Weight 638.8 g/mol
Molecular Formula C36H46N8O3
XLogP33.1
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count6
Rotatable Bond Count6
Exact Mass638.36928736 g/mol
Monoisotopic Mass638.36928736 g/mol
Topological Polar Surface Area117 Ų
Heavy Atom Count47
Formal Charge0
Complexity1160
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1

API SUPPLIERS

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Moehs Iberica

Spain

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Metrochem API Private Limited

India

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Axplora

Germany

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Farmhispania

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Jinan Tantu Chemicals

China

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Saptagir Laboratories

India

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Zhejiang Tianyu Pharmaceutical Co....

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Micro Labs Limited

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API Reference Price

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28-Mar-2024
28-Mar-2024
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Drugs in Development

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Details:

Pfizer has given Royalty Pharma an accelerated milestone payment following the US approval of its migraine nasal spray, Zavzpret (zavegepant). Zavzpret was approved by the U.S. FDA, which provides another important new treatment option for migraine patients.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: Zavzpret

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Pfizer Inc

Deal Size: $475.0 million Upfront Cash: Undisclosed

Deal Type: Agreement March 15, 2023

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01

PharmaVenue
Not Confirmed
PharmaVenue
Not Confirmed

Details : Pfizer has given Royalty Pharma an accelerated milestone payment following the US approval of its migraine nasal spray, Zavzpret (zavegepant). Zavzpret was approved by the U.S. FDA, which provides another important new treatment option for migraine patie...

Brand Name : Zavzpret

Molecule Type : Small molecule

Upfront Cash : Undisclosed

March 15, 2023

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Details:

Zavzpret (zavegepant) is a calcitonin gene-related peptide receptor antagonist. CGRP antagonists have been shown pain relief during migraine induced headaches.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: Zavzpret

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 10, 2023

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02

Pfizer Inc

U.S.A
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PharmaVenue
Not Confirmed

Pfizer Inc

U.S.A
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PharmaVenue
Not Confirmed

Details : Zavzpret (zavegepant) is a calcitonin gene-related peptide receptor antagonist. CGRP antagonists have been shown pain relief during migraine induced headaches.

Brand Name : Zavzpret

Molecule Type : Small molecule

Upfront Cash : Not Applicable

March 10, 2023

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Details:

Complete data from the Phase 3 BHV3500 (zavegepant) nasal spray study highlight its ultra-rapid pain relief in as little as 15 minutes that lasts through 48 hours after a single dose.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: BHV-3500

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 13, 2022

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03

PharmaVenue
Not Confirmed
PharmaVenue
Not Confirmed

Details : Complete data from the Phase 3 BHV3500 (zavegepant) nasal spray study highlight its ultra-rapid pain relief in as little as 15 minutes that lasts through 48 hours after a single dose.

Brand Name : BHV-3500

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 13, 2022

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Details:

In the pivotal studies, BHV3500 (zavegepant) was statistically superior to placebo on the coprimary regulatory endpoints of superiority to placebo at 2 hours for pain freedom and freedom from the migraine-associated most bothersome.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: BHV-3500

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 23, 2022

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04

PharmaVenue
Not Confirmed
PharmaVenue
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Details : In the pivotal studies, BHV3500 (zavegepant) was statistically superior to placebo on the coprimary regulatory endpoints of superiority to placebo at 2 hours for pain freedom and freedom from the migraine-associated most bothersome.

Brand Name : BHV-3500

Molecule Type : Small molecule

Upfront Cash : Not Applicable

May 23, 2022

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Details:

Biohaven plans to file a NDA for BHV-3500 (zavegepant) with the USFDA in 1Q2022,showed ultra-rapid pain relief at the earliest measured time point of 15 minutes and sustained efficacy through 48 hours after a single intranasal dose.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: BHV-3500

Study Phase: Phase II/ Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 06, 2021

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05

PharmaVenue
Not Confirmed
PharmaVenue
Not Confirmed

Details : Biohaven plans to file a NDA for BHV-3500 (zavegepant) with the USFDA in 1Q2022,showed ultra-rapid pain relief at the earliest measured time point of 15 minutes and sustained efficacy through 48 hours after a single intranasal dose.

Brand Name : BHV-3500

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 06, 2021

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Details:

Zavegepant is a high affinity, selective and structurally unique, third generation, CGRP receptor antagonist in development for both migraine and non-migraine CGRP-mediated diseases.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: BHV-3500

Study Phase: Phase II/ Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 29, 2021

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06

PharmaVenue
Not Confirmed
PharmaVenue
Not Confirmed

Details : Zavegepant is a high affinity, selective and structurally unique, third generation, CGRP receptor antagonist in development for both migraine and non-migraine CGRP-mediated diseases.

Brand Name : BHV-3500

Molecule Type : Small molecule

Upfront Cash : Not Applicable

March 29, 2021

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Details:

Zavegepant is a third generation, high affinity, selective and structurally unique, small molecule CGRP receptor antagonist in development for both migraine and non-migraine indications including COVID-19 associated lung inflammation.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: BHV-3500

Study Phase: Phase II/ Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 10, 2020

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07

PharmaVenue
Not Confirmed
PharmaVenue
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Details : Zavegepant is a third generation, high affinity, selective and structurally unique, small molecule CGRP receptor antagonist in development for both migraine and non-migraine indications including COVID-19 associated lung inflammation.

Brand Name : BHV-3500

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 10, 2020

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Details:

Funding will advance the Biohaven's CGRP receptor antagonist program through the development of zavegepant (vazegepant). The zavegepant program encompasses intranasal zavegepant as well as oral zavegepant for migraine prevention and non-migraine indications.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: BHV-3500

Study Phase: Phase II/ Phase IIIProduct Type: Small molecule

Sponsor: Royalty Pharma

Deal Size: $450.0 million Upfront Cash: Undisclosed

Deal Type: Funding August 07, 2020

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PharmaVenue
Not Confirmed
PharmaVenue
Not Confirmed

Details : Funding will advance the Biohaven's CGRP receptor antagonist program through the development of zavegepant (vazegepant). The zavegepant program encompasses intranasal zavegepant as well as oral zavegepant for migraine prevention and non-migraine indicati...

Brand Name : BHV-3500

Molecule Type : Small molecule

Upfront Cash : Undisclosed

August 07, 2020

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Details:

Biohaven plans to study intranasal vazegepant, a high affinity, selective and structurally unique, small molecule CGRP receptor antagonist, in pulmonary complications of COVID-19 disease.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Infections and Infectious Diseases Brand Name: BHV-3500

Study Phase: Phase II/ Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable April 09, 2020

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09

PharmaVenue
Not Confirmed
PharmaVenue
Not Confirmed

Details : Biohaven plans to study intranasal vazegepant, a high affinity, selective and structurally unique, small molecule CGRP receptor antagonist, in pulmonary complications of COVID-19 disease.

Brand Name : BHV-3500

Molecule Type : Small molecule

Upfront Cash : Not Applicable

April 09, 2020

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Details:

The Company addressed all issues raised by the FDA and will advance the 10 mg dose of intranasal vazegepant into a double-blind, placebo-controlled Phase 3 clinical trial.


Lead Product(s): Zavegepant HCl

Therapeutic Area: Neurology Brand Name: BHV-3500

Study Phase: Phase II/ Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 23, 2020

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10

PharmaVenue
Not Confirmed
PharmaVenue
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Details : The Company addressed all issues raised by the FDA and will advance the 10 mg dose of intranasal vazegepant into a double-blind, placebo-controlled Phase 3 clinical trial.

Brand Name : BHV-3500

Molecule Type : Small molecule

Upfront Cash : Not Applicable

March 23, 2020

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FDF Dossiers

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Pfizer Inc

U.S.A
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Pfizer Inc

U.S.A
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ZAVEGEPANT HYDROCHLORIDE

Brand Name : ZAVZPRET

Dosage Form : SPRAY, METERED;NASAL

Dosage Strength : EQ 10MG BASE/SPRAY

Packaging :

Approval Date : 2023-03-09

Application Number : 216386

Regulatory Info : RX

Registration Country : USA

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Patents & EXCLUSIVITIES

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US Patents

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PFIZER

U.S.A
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ZAVEGEPANT HYDROCHLORIDE

US Patent Number : 7220862

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 216386

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2024-01-21

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PFIZER

U.S.A
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ZAVEGEPANT HYDROCHLORIDE

US Patent Number : 8481546

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 216386

Patent Use Code : U-3555

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2031-10-07

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ABOUT THIS PAGE

Zavegepant HCl Manufacturers

A Zavegepant HCl manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Zavegepant HCl, including repackagers and relabelers. The FDA regulates Zavegepant HCl manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Zavegepant HCl API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

click here to find a list of Zavegepant HCl manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Zavegepant HCl Suppliers

A Zavegepant HCl supplier is an individual or a company that provides Zavegepant HCl active pharmaceutical ingredient (API) or Zavegepant HCl finished formulations upon request. The Zavegepant HCl suppliers may include Zavegepant HCl API manufacturers, exporters, distributors and traders.

click here to find a list of Zavegepant HCl suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Zavegepant HCl NDC

National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Zavegepant HCl as an active pharmaceutical ingredient (API).

Finished drug products

The FDA updates the NDC directory daily. The NDC numbers for Zavegepant HCl API and other APIs are published in this directory by the FDA.

Unfinished drugs

The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

Pharmaceutical companies that manufacture Zavegepant HCl as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

Compounded drug products

The NDC directory also contains data on finished compounded human drug products that contain Zavegepant HCl and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Zavegepant HCl NDC to their finished compounded human drug products, they may choose to do so.

click here to find a list of Zavegepant HCl suppliers with NDC on PharmaCompass.

Zavegepant HCl GMP

Zavegepant HCl Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Zavegepant HCl GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Zavegepant HCl GMP manufacturer or Zavegepant HCl GMP API supplier for your needs.

Zavegepant HCl CoA

A Zavegepant HCl CoA (Certificate of Analysis) is a formal document that attests to Zavegepant HCl's compliance with Zavegepant HCl specifications and serves as a tool for batch-level quality control.

Zavegepant HCl CoA mostly includes findings from lab analyses of a specific batch. For each Zavegepant HCl CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Zavegepant HCl may be tested according to a variety of international standards, such as European Pharmacopoeia (Zavegepant HCl EP), Zavegepant HCl JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Zavegepant HCl USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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