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Atogepant

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Chemistry

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Also known as: Qulipta, Mk-8031, 1374248-81-3, Agn-241689, Atogepant [inn], Atogepant [who-dd]

Molecular Formula

C₂₉H₂₃F₆N₅O₃

Molecular Weight

603.5 g/mol

InChI Key

QIVUCLWGARAQIO-OLIXTKCUSA-N

FDA UNII

7CRV8RR151

Atogepant is an oral antagonist of calcitonin gene-related peptide (CGRP) receptors indicated for the prevention of episodic migraine headaches. It was developed by AbbVie and received FDA approval under the brand name Qulipta in September 2021. While its approval was predated by two other members of the same drug family, namely [ubrogepant] and [rimegepant], these agents are indicated only for abortive migraine therapy - atogepant is novel in that it is the first and only oral CGRP antagonist approved for preventative use in migraine. In patients requiring preventative migraine therapy, current practice guidelines recommend the use of certain anti-epileptic medications (e.g. [valproic acid] or [topiramate]) or beta-blockers (e.g. [propranolol]), all of which can be associated with significant adverse effects. The "gepants" family of drugs, including atogepant, are comparatively well-tolerated and may provide a desirable treatment option for patients struggling with adverse reactions to other preventative therapies.

Atogepant is a Calcitonin Gene-related Peptide Receptor Antagonist. The mechanism of action of atogepant is as a Calcitonin Gene-related Peptide Receptor Antagonist.

1 2D Structure

Atogepant

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(3S)-N-[(3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl]-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6'-5,7-dihydrocyclopenta[b]pyridine]-3'-carboxamide

2.1.2 InChI

InChI=1S/C29H23F6N5O3/c1-13-16(22-18(30)4-5-19(31)23(22)32)8-20(26(42)40(13)12-29(33,34)35)38-25(41)15-7-14-9-28(10-21(14)37-11-15)17-3-2-6-36-24(17)39-27(28)43/h2-7,11,13,16,20H,8-10,12H2,1H3,(H,38,41)(H,36,39,43)/t13-,16-,20+,28+/m1/s1

2.1.3 InChI Key

QIVUCLWGARAQIO-OLIXTKCUSA-N

2.1.4 Canonical SMILES

CC1C(CC(C(=O)N1CC(F)(F)F)NC(=O)C2=CC3=C(CC4(C3)C5=C(NC4=O)N=CC=C5)N=C2)C6=C(C=CC(=C6F)F)F

2.1.5 Isomeric SMILES

C[C@@H]1[C@@H](C[C@@H](C(=O)N1CC(F)(F)F)NC(=O)C2=CC3=C(C[C@@]4(C3)C5=C(NC4=O)N=CC=C5)N=C2)C6=C(C=CC(=C6F)F)F

2.2 Other Identifiers

2.2.1 UNII

7CRV8RR151

2.3 Synonyms

2.3.1 MeSH Synonyms

1. (3s)-n-((3s,5s,6r)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl)-2-oxospiro(1h-pyrrolo(2,3-b)pyridine-3,6'-5,7-dihydrocyclopenta(b)pyridine)-3'-carboxamide

2.3.2 Depositor-Supplied Synonyms

1. Qulipta

2. Mk-8031

3. 1374248-81-3

4. Agn-241689

5. Atogepant [inn]

6. Atogepant [who-dd]

7. 7crv8rr151

8. Atogepant (usan)

9. Atogepant [usan]

10. (3's)-1',2',5,7-tetrahydro-n-((3s,5s,6r)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)-3-piperidinyl)-2'-oxospiro(6h-cyclopenta(b)pyridine-6,3'-(3h)pyrrolo(2,3-b)pyridine)-3-carboxamide

11. (3's)-n-[(3s,5s,6r)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl]-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamide

12. (3s)-n-[(3s,5s,6r)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl]-2-oxospiro[1h-pyrrolo[2,3-b]pyridine-3,6'-5,7-dihydrocyclopenta[b]pyridine]-3'-carboxamide

13. Spiro(6h-cyclopenta(b)pyridine-6,3'-(3h)pyrrolo(2,3-b)pyridine)-3-carboxamide, 1',2',5,7-tetrahydro-n-((3s,5s,6r)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)-3-piperidinyl)-2'-oxo-, (3's)-

14. Atogepant [usan:inn]

15. Unii-7crv8rr151

16. Gtpl9730

17. Schembl4570348

18. Atogepant [orange Book]

19. Chembl3991065

20. Dtxsid901337079

21. Bcp29018

22. Ex-a6847

23. Mk 8031; Mk8031; Atogepant

24. Example 4 [us20120122911]

25. Hy-109022

26. Cs-0030524

27. D11313

2.4 Create Date

2013-12-02

3 Chemical and Physical Properties

Molecular Formula	C₂₉H₂₃F₆N₅O₃
Molecular Weight	603.5 g/mol
XLogP3	3.4
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	11
Rotatable Bond Count	4
Exact Mass	603.17050859 g/mol
Monoisotopic Mass	603.17050859 g/mol
Topological Polar Surface Area	104 Å²
Heavy Atom Count	43
Formal Charge	0
Complexity	1110
Isotope Atom Count	0
Defined Atom Stereocenter Count	4
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

Atogepant is indicated for the prevention of episodic migraine in adults.

Prevention of migraine headaches

5 Pharmacology and Biochemistry

5.1 Pharmacology

Atogepant helps to prevent migraine headaches by antagonizing the activity of a pronociceptive molecule (CGRP) which has been implicated in migraine pathophysiology. Intended for preventative use, rather than abortive migraine therapy, atogepant is administered once daily. While no dose adjustments are required for patients with mild or moderate hepatic impairment, atogepant should be avoided in patients with severe hepatic impairment. Similarly, no dose adjustments are required for patients with mild or moderate renal impairment, but patients with severe renal impairment should be limited to a maximum daily dose of 10mg.

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

ATOGEPANT

5.2.2 FDA UNII

7CRV8RR151

5.2.3 Pharmacological Classes

Calcitonin Gene-related Peptide Receptor Antagonists [MoA]; Calcitonin Gene-related Peptide Receptor Antagonist [EPC]

5.3 ATC Code

N - Nervous system

N02 - Analgesics

N02C - Antimigraine preparations

N02CD - Calcitonin gene-related peptide (cgrp) antagonists

N02CD07 - Atogepant

5.4 Absorption, Distribution and Excretion

Absorption

The time to peak plasma concentration following oral administration is approximately 2-3 hours. Atogepant displays dose-proportional pharmacokinetics up to approximately 3-fold its recommended maximum dosage, and its pharmacokinetics are not significantly influenced by co-administration with food.

Route of Elimination

The elimination of atogepant occurs primarily via metabolism by CYP3A4. Following a single oral dose of radiolabeled atogepant to healthy male subjects, 42% of the administered dose was recovered as unchanged parent drug in the feces and 5% as unchanged parent drug in the urine. In total, approximately 81% of the radioactivity was recovered in the feces, with only 8% recovered in the urine.

Volume of Distribution

The mean apparent volume of distribution of atogepant is 292 L.

Clearance

The mean apparent oral clearance of atogepant is approximately 19 L/h.

5.5 Metabolism/Metabolites

The metabolism of atogepant is mediated primarily via CYP3A4. The most prevalent circulating compounds in plasma are atogepant itself and a glucuronide conjugate metabolite (M23), comprising approximately 75% and 15% of the administered dose, respectively, with at least 10 other metabolites detected in feces representing <10% of the administered dose.

5.6 Biological Half-Life

The elimination half-life of atogepant following oral administration is approximately 11 hours.

5.7 Mechanism of Action

The currently accepted theory of migraine pathophysiology considers dysfunction of the central nervous system, in particular the trigeminal ganglion, to be the root cause behind the condition. Activation of the trigeminal ganglion triggers the stimulation of trigeminal afferents that project to the spinal cord and synapse on various pain-sensing intra- and extracranial structures, such as the dura mater. Pain signals are then further transmitted via second-order ascending neurons to the brainstem, hypothalamus, and thalamic nuclei, and from there to several cortical regions (e.g. auditory, visual, motor cortices). The trigeminal ganglion appears to amplify and perpetuate the migraine headache pain through the activation of perivascular fibers and the release of molecules involved in pain generation, such as calcitonin gene-related peptide (CGRP). The -isoform of CGRP, expressed in primary sensory neurons, is a potent vasodilator and has been implicated in migraine pathogenesis - CGRP levels are acutely elevated during migraine attacks, return to normal following treatment with triptan medications, and intravenous infusions of CGRP have been shown to trigger migraine-like headaches in migraine patients. In addition to its vasodilatory properties, CGRP appears to be a pronociceptive factor that modulates neuronal excitability to facilitate pain responses. Atogepant is an antagonist of the calcitonin gene-related peptide receptor - it competes with CGRP for occupancy at these receptors, preventing the actions of CGRP and its ability to induce and perpetuate migraine headache pain.

API SUPPLIERS

01

Metrochem API Private Limited

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

Pharmtech & Ingredients

Exhibiting

Metrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.

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India

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USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT

02

MSN Laboratories

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

AusBiotech 2024

Not Confirmed

03

Micro Labs Limited

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

AusBiotech 2024

Not Confirmed

04

Hebi Xinhe Pharmaceutical

China

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

AusBiotech 2024

Not Confirmed

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Listed Suppliers

01

Metrochem API Private Limited

India

Pharmtech & Ingredients

Exhibiting

Metrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.

Contact Supplier

India

Virtual Booth

Digital Content

Atogepant

About the Company :

Established in 2004, Metrochem API is one of the fastest-growing APIs, pellets & intermediates manufacturers. It has 6 dedicated manufacturing facilities for its 3 core product ...

Established in 2004, Metrochem API is one of the fastest-growing APIs, pellets & intermediates manufacturers. It has 6 dedicated manufacturing facilities for its 3 core product groups and has been approved by ISO 9001-2015, USFDA, WHO GMP, Cofepris & Japanese authorities. Metrochem’s in-depth industry knowledge, & hi-tech & advanced infrastructure, helps it provide quality products to its customers. Note: None of the products will be supplied to the countries where this could conflict with existing patents. Further, any products under patent will be offered for R&D purposes only. However, the final responsibility lies with the buyer