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Chemistry

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Also known as: Clazosentan disodium, Clazosentan disodium salt, Clazosentan sodium [jan], Clazosentan disodium salt [mi], 0l77pk62l1, 503271-02-1
Molecular Formula
C25H21N9Na2O6S
Molecular Weight
621.5  g/mol
InChI Key
PZNSONUYVNYXJZ-UHFFFAOYSA-N
FDA UNII
0L77PK62L1

Clazosentan Sodium
1 2D Structure

Clazosentan Sodium

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
disodium;[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)pyridin-4-yl]pyrimidin-4-yl]-(5-methylpyridin-2-yl)sulfonylazanide
2.1.2 InChI
InChI=1S/C25H21N9O6S.2Na/c1-15-7-8-20(27-14-15)41(36,37)32-24-21(40-19-6-4-3-5-18(19)38-2)25(39-12-11-35)29-22(28-24)16-9-10-26-17(13-16)23-30-33-34-31-23;;/h3-10,13-14,35H,11-12H2,1-2H3;;/q-2;2*+1
2.1.3 InChI Key
PZNSONUYVNYXJZ-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC1=CN=C(C=C1)S(=O)(=O)[N-]C2=C(C(=NC(=N2)C3=CC(=NC=C3)C4=NN=N[N-]4)OCCO)OC5=CC=CC=C5OC.[Na+].[Na+]
2.2 Other Identifiers
2.2.1 UNII
0L77PK62L1
2.3 Synonyms
2.3.1 Depositor-Supplied Synonyms

1. Clazosentan Disodium

2. Clazosentan Disodium Salt

3. Clazosentan Sodium [jan]

4. Clazosentan Disodium Salt [mi]

5. 0l77pk62l1

6. 503271-02-1

7. 2-pyridinesulfonamide, N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-(1h-tetrazol-5-yl)-4-pyridinyl)-4-pyrimidinyl)-5-methyl-, Disodium Salt

8. Unii-0l77pk62l1

9. Dtxsid10198341

10. Q27236935

2.4 Create Date
2011-05-05
3 Chemical and Physical Properties
Molecular Weight 621.5 g/mol
Molecular Formula C25H21N9Na2O6S
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count15
Rotatable Bond Count11
Exact Mass621.11308916 g/mol
Monoisotopic Mass621.11308916 g/mol
Topological Polar Surface Area183 Ų
Heavy Atom Count43
Formal Charge0
Complexity911
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count3

Drugs in Development

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Details:

Handok is responsible for commercialization of Pivlaz (clazosentan sodium), approved in South Korea for preventing cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage.


Lead Product(s): Clazosentan Sodium

Therapeutic Area: Neurology Brand Name: Pivlaz

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: HANDOK

Deal Size: Undisclosed Upfront Cash: Undisclosed

Deal Type: Agreement April 14, 2024

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01

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : Handok is responsible for commercialization of Pivlaz (clazosentan sodium), approved in South Korea for preventing cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage.

Brand Name : Pivlaz

Molecule Type : Small molecule

Upfront Cash : Undisclosed

April 14, 2024

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Details:

South Korea approved PIVLAZ™ (clazosentan sodium), an ETAR antagonist, for the prevention of cerebral vasospasm, vasospasm-related cerebral infarction, and cerebral ischemic symptoms after aneurysmal subarachnoid hemorrhage (aSAH) securing.


Lead Product(s): Clazosentan Sodium

Therapeutic Area: Neurology Brand Name: Pivlaz

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 07, 2023

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02

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : South Korea approved PIVLAZ™ (clazosentan sodium), an ETAR antagonist, for the prevention of cerebral vasospasm, vasospasm-related cerebral infarction, and cerebral ischemic symptoms after aneurysmal subarachnoid hemorrhage (aSAH) securing.

Brand Name : Pivlaz

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 07, 2023

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Details:

Through the acquisition, Sosei also gains assignment of Pivlaz (clazosentan), for the treatment of cerebral vasospasm, and license rights to daridorexant in the Asia Pacific (ex-China) region.


Lead Product(s): Clazosentan Sodium

Therapeutic Area: Neurology Brand Name: Pivlaz

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Sosei Heptares

Deal Size: Undisclosed Upfront Cash: Undisclosed

Deal Type: Acquisition July 20, 2023

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03

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : Through the acquisition, Sosei also gains assignment of Pivlaz (clazosentan), for the treatment of cerebral vasospasm, and license rights to daridorexant in the Asia Pacific (ex-China) region.

Brand Name : Pivlaz

Molecule Type : Small molecule

Upfront Cash : Undisclosed

July 20, 2023

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Details:

ACT-108475 (clazosentan) is a fast-acting, endothelin A (ETA) receptor antagonist, that Idorsia has developed as a continuous intravenous infusion for the prevention of clinical deterioration due to delayed cerebral ischemia (DCI) in patients following aSAH.


Lead Product(s): Clazosentan Sodium

Therapeutic Area: Neurology Brand Name: ACT-108475

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable February 06, 2023

blank

04

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : ACT-108475 (clazosentan) is a fast-acting, endothelin A (ETA) receptor antagonist, that Idorsia has developed as a continuous intravenous infusion for the prevention of clinical deterioration due to delayed cerebral ischemia (DCI) in patients following a...

Brand Name : ACT-108475

Molecule Type : Small molecule

Upfront Cash : Not Applicable

February 06, 2023

blank

Details:

PIVLAZ (clazosentan sodium), a selective endothelin A receptor antagonist received Japanese PMDA approval on the basis of statistically significant result from the Japanese Phase 3 program for the prevention of cerebral vasospasm after subarachnoid hemorrhage treatment.


Lead Product(s): Clazosentan Sodium

Therapeutic Area: Neurology Brand Name: Pivlaz

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable January 20, 2022

blank

05

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : PIVLAZ (clazosentan sodium), a selective endothelin A receptor antagonist received Japanese PMDA approval on the basis of statistically significant result from the Japanese Phase 3 program for the prevention of cerebral vasospasm after subarachnoid hemor...

Brand Name : Pivlaz

Molecule Type : Small molecule

Upfront Cash : Not Applicable

January 20, 2022

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Details:

A Phase 2 study in Japanese and Korean patients showed that 10 mg/hr of clazosentan administered by continuous intravenous infusion significantly reduced vasospasm and vasospasm-related morbidity and mortality events.


Lead Product(s): Clazosentan Sodium

Therapeutic Area: Neurology Brand Name: ACT-108475

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 01, 2021

blank

06

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : A Phase 2 study in Japanese and Korean patients showed that 10 mg/hr of clazosentan administered by continuous intravenous infusion significantly reduced vasospasm and vasospasm-related morbidity and mortality events.

Brand Name : ACT-108475

Molecule Type : Small molecule

Upfront Cash : Not Applicable

March 01, 2021

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Details:

Both studies demonstrated that clazosentan reduced the occurrence of cerebral vasospasm-related morbidity and all-cause mortality within 6 weeks post-aSAH with statistical significance (p<0.01 for both studies).


Lead Product(s): Clazosentan Sodium

Therapeutic Area: Neurology Brand Name: ACT-108475

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 23, 2020

blank

07

Medlab Asia & Asia Health
Not Confirmed
Medlab Asia & Asia Health
Not Confirmed

Details : Both studies demonstrated that clazosentan reduced the occurrence of cerebral vasospasm-related morbidity and all-cause mortality within 6 weeks post-aSAH with statistical significance (p<0.01 for both studies).

Brand Name : ACT-108475

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 23, 2020

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NEWS #PharmaBuzz

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https://www.biospectrumasia.com/news/25/24084/nxera-pharma-inks-deal-with-handok-to-distribute-pivlaz-in-south-korea.html

BIOSPECTRUM ASIA
16 Apr 2024

https://www.globenewswire.com/news-release/2024/04/14/2862478/0/en/Nxera-Pharma-Announces-Exclusive-Supply-and-Distribution-Agreement-with-Handok-for-PIVLAZ-in-South-Korea.html

GLOBENEWSWIRE
14 Apr 2024

https://www.globenewswire.com//news-release/2023/12/07/2792220/0/en/Sosei-Group-Announces-Marketing-Approval-for-PIVLAZ-clazosentan-sodium-150-mg-in-South-Korea.html

GLOBENEWSWIRE
07 Dec 2023

https://www.globenewswire.com/news-release/2023/02/06/2601762/0/de/Idorsia-announces-th[…]patients-following-aneurysmal-subarachnoid-hemorrhage.html

GLOBENEWSWIRE
07 Feb 2023

https://www.globenewswire.com/news-release/2022/04/20/2425136/0/de/PIVLAZ-clazosentan-Idorsia-s-first-commercial-product-now-available-for-patients-in-Japan.html

GLOBENEWSWIRE
20 Apr 2022

https://www.globenewswire.com/news-release/2022/04/04/2415246/0/de/The-Journal-of-Neurosurgery-reports-impact-of-clazosentan-on-cerebral-vasospasm-related-morbidity-and-all-cause-mortality-after-aneurysmal-subarachnoid-hemorrhage.html

GLOBENEWSWIRE
04 Apr 2022

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