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Synopsis

Synopsis

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Chemistry

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Also known as: Azd5363, 1143532-39-1, Azd-5363, Azd 5363, (s)-4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
Molecular Formula
C21H25ClN6O2
Molecular Weight
428.9  g/mol
InChI Key
JDUBGYFRJFOXQC-KRWDZBQOSA-N
FDA UNII
WFR23M21IE

Capivasertib
Capivasertib is a novel pyrrolopyrimidine derivative, and an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. Capivasertib binds to and inhibits all AKT isoforms. Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism. A wide range of solid and hematological malignancies show dysregulated PI3K/AKT/mTOR signaling due to mutations in multiple signaling components. By targeting AKT, the key node in the PIK3/AKT signaling network, this agent may be used as monotherapy or combination therapy for a variety of human cancers.
1 2D Structure

Capivasertib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
2.1.2 InChI
InChI=1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1
2.1.3 InChI Key
JDUBGYFRJFOXQC-KRWDZBQOSA-N
2.1.4 Canonical SMILES
C1CN(CCC1(C(=O)NC(CCO)C2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4
2.1.5 Isomeric SMILES
C1CN(CCC1(C(=O)N[C@@H](CCO)C2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4
2.2 Other Identifiers
2.2.1 UNII
WFR23M21IE
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)piperidine-4-carboxamide

2. Azd5363

2.3.2 Depositor-Supplied Synonyms

1. Azd5363

2. 1143532-39-1

3. Azd-5363

4. Azd 5363

5. (s)-4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide

6. 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide

7. Wfr23m21ie

8. 4-piperidinecarboxamide, 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-

9. 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide

10. Unii-wfr23m21ie

11. Chembl2325741

12. Cc-638

13. Capivasertib?

14. 4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)piperidine-4-carboxamide

15. 4-piperidinecarboxamide, 4-amino-n-((1s)-1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-

16. Capivasertib (jan/usan)

17. Capivasertib [inn]

18. Capivasertib [jan]

19. Capivasertib [usan]

20. Capivasertib (azd5363)

21. Mls006011179

22. Capivasertib [who-dd]

23. Schembl390243

24. Gtpl7709

25. Azc5363

26. Dtxsid40150710

27. Ex-a285

28. Us10654855, Example 9

29. Bdbm443385

30. Mfcd22628785

31. Nsc764039

32. Nsc782347

33. Nsc799347

34. S8019

35. Zinc43204023

36. Akos027323693

37. Bcp9000365

38. Ccg-268989

39. Cs-1284

40. Db12218

41. Nsc-764039

42. Nsc-782347

43. Nsc-799347

44. Ncgc00345795-01

45. Ncgc00345795-04

46. Ac-32685

47. Hy-15431

48. Smr004702948

49. Bcp0726000111

50. A1387

51. Sw220158-1

52. D11371

53. J-514447

54. Q27074756

55. 0xz

56. 4-amino-n-((1s)-1-(4-chlorophenyl)-3-hydroxypropyl)-1- (1h-pyrrolo(2,3-d)pyrimidin-4-yl)piperidine-4-carboxamide

57. Alternative Route 1: (s)-4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide

2.4 Create Date
2009-04-28
3 Chemical and Physical Properties
Molecular Weight 428.9 g/mol
Molecular Formula C21H25ClN6O2
XLogP31.7
Hydrogen Bond Donor Count4
Hydrogen Bond Acceptor Count6
Rotatable Bond Count6
Exact Mass428.1727518 g/mol
Monoisotopic Mass428.1727518 g/mol
Topological Polar Surface Area120 Ų
Heavy Atom Count30
Formal Charge0
Complexity580
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Treatment of breast cancer , Treatment of prostate cancer


API SUPPLIERS

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01

Chongqing Sintaho Pharmaceutical

China

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

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Medlab Asia & Asia Health
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  • fda
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  • WHO-GMP

Virtual BoothChongqing Sintaho Pharma: A trusted partner globally for chemosynthetic APIs.

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USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT
Chongqing Sintaho Pharmaceutical
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Listed Suppliers

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Virtual BoothChongqing Sintaho Pharma: A trusted partner globally for chemosynthetic APIs.

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Capivasertib

About the Company : Sintaho Pharmaceutical Co., Ltd., located in Chongqing, China, contributes to being the most dependable partner for global pharmaceutical companies. Sintaho specializes in chemosyn...

Sintaho Pharmaceutical Co., Ltd., located in Chongqing, China, contributes to being the most dependable partner for global pharmaceutical companies. Sintaho specializes in chemosynthetic APIs (application contains oncology, nervous system, and metabolic diseases and etc.,) with a product portfolio ranging from small molecule APIs, ADC compounds (linkers and payloads) to polypeptides, also provides CDMO services of cytotoxic and OEB4/5 grade APIs.
Chongqing Sintaho Pharmaceutical

02

Capivasertib

About the Company : Founded in 1935, TAPI Technology & API Services has a long-standing tradition of advancing health through innovation and dedication. Today, we proudly build upon this legacy, drivi...

Founded in 1935, TAPI Technology & API Services has a long-standing tradition of advancing health through innovation and dedication. Today, we proudly build upon this legacy, driving progress in the pharmaceutical industry. Leveraging our extensive experience and world-class expertise, we deliver one of the most comprehensive API portfolios in the industry. Additionally, we provide tailored CDMO services, harnessing our proficiency in diverse technologies to meet our partners' unique needs, ensuring flexibility and excellence in every project.
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Drugs in Development

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Details:

Truqap (capivasertib) is a first-in-class, potent, ATP-competitive inhibitor of AKT1/2/3. It is being evaluated for the treatment of locally advanced or metastatic triple-negative breast cancer.


Lead Product(s): Capivasertib,Paclitaxel

Therapeutic Area: Oncology Brand Name: Truqap

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 18, 2024

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01

AstraZeneca

United Kingdom
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Medlab Asia & Asia Health
Not Confirmed

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Truqap (capivasertib) is a first-in-class, potent, ATP-competitive inhibitor of AKT1/2/3. It is being evaluated for the treatment of locally advanced or metastatic triple-negative breast cancer.

Brand Name : Truqap

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 18, 2024

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Details:

Truqap (capivasertib) is a first-in-class AKT inhibitor approved in combination with fulvestrant for advanced HR-positive breast cancer treatment.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: Truqap

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable April 29, 2024

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02

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Truqap (capivasertib) is a first-in-class AKT inhibitor approved in combination with fulvestrant for advanced HR-positive breast cancer treatment.

Brand Name : Truqap

Molecule Type : Small molecule

Upfront Cash : Not Applicable

April 29, 2024

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Details:

Truqap (capivasertib) is a first-in-class ATP-competitive inhibitor of all three AKT isoforms, approved with Faslodex (fulvestrant) for advanced HER2-/HR+ breast cancer treatment.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: Truqap

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: AstraZeneca

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 27, 2024

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03

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

Details : Truqap (capivasertib) is a first-in-class ATP-competitive inhibitor of all three AKT isoforms, approved with Faslodex (fulvestrant) for advanced HER2-/HR+ breast cancer treatment.

Brand Name : Truqap

Molecule Type : Small molecule

Upfront Cash : Not Applicable

March 27, 2024

blank

Details:

Truqap (capivasertib) is an ATP-competitive inhibitor of all AKT isoforms, approved in combination with Faslodex (fulvestrant) for advanced HR-positive breast cancer treatment.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: Truqap

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 27, 2024

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04

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Truqap (capivasertib) is an ATP-competitive inhibitor of all AKT isoforms, approved in combination with Faslodex (fulvestrant) for advanced HR-positive breast cancer treatment.

Brand Name : Truqap

Molecule Type : Small molecule

Upfront Cash : Not Applicable

March 27, 2024

blank

Details:

Truqap, a first-in-class AKT inhibitor, discovered by AstraZeneca subsequent to its collaboration with Astex, recently approved by FDA in combination with Faslodex, for treatment for adult patients with HR-positive, HER2-negative, locally advanced or metastatic breast cancer.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: Truqap

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: AstraZeneca

Deal Size: $275.0 million Upfront Cash: $5.0 million

Deal Type: Collaboration November 22, 2023

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05

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

Details : Truqap, a first-in-class AKT inhibitor, discovered by AstraZeneca subsequent to its collaboration with Astex, recently approved by FDA in combination with Faslodex, for treatment for adult patients with HR-positive, HER2-negative, locally advanced or met...

Brand Name : Truqap

Molecule Type : Small molecule

Upfront Cash : $5.0 million

November 22, 2023

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Details:

Truqap (capivasertib), a first in class, oral targeted inhibitor of the cancer-driving protein AKT, was discovered by AstraZeneca subsequent to its discovery collaboration with Astex.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: Truqap

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: AstraZeneca

Deal Size: $275.0 million Upfront Cash: $5.0 million

Deal Type: Collaboration November 20, 2023

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06

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

Details : Truqap (capivasertib), a first in class, oral targeted inhibitor of the cancer-driving protein AKT, was discovered by AstraZeneca subsequent to its discovery collaboration with Astex.

Brand Name : Truqap

Molecule Type : Small molecule

Upfront Cash : $5.0 million

November 20, 2023

blank

Details:

Truqap (capivasertib) is a first-in-class, potent, ATP-competitive inhibitor of all three AKT isoforms (AKT1/2/3). It is approved in combination with fulvestrant for the treatment of patients with advanced HR-positive breast cancer.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: Truqap

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 20, 2023

blank

07

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

Details : Truqap (capivasertib) is a first-in-class, potent, ATP-competitive inhibitor of all three AKT isoforms (AKT1/2/3). It is approved in combination with fulvestrant for the treatment of patients with advanced HR-positive breast cancer.

Brand Name : Truqap

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 20, 2023

blank

Details:

Truqap (capivasertib) is a first-in-class, potent, ATP-competitive inhibitor of all three AKT isoforms (AKT1/2/3). It is approved in combination with fulvestrant for the treatment of patients with advanced HR-positive breast cancer.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: Truqap

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 17, 2023

blank

08

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Truqap (capivasertib) is a first-in-class, potent, ATP-competitive inhibitor of all three AKT isoforms (AKT1/2/3). It is approved in combination with fulvestrant for the treatment of patients with advanced HR-positive breast cancer.

Brand Name : Truqap

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 17, 2023

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Details:

AZD5363 (capivasertib) is an investigational orally and potent, adenosine triphosphate (ATP)-competitive inhibitor of all three AKT isoforms (AKT1/2/3) and in combination with Faslodex granted Priority Review in the US for patients with advanced HR-positive breast cancer.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: AZD5363

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 12, 2023

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09

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : AZD5363 (capivasertib) is an investigational orally and potent, adenosine triphosphate (ATP)-competitive inhibitor of all three AKT isoforms (AKT1/2/3) and in combination with Faslodex granted Priority Review in the US for patients with advanced HR-posit...

Brand Name : AZD5363

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 12, 2023

blank

Details:

Capivasertib (AZD 5363), is an investigational oral treatment currently in Phase III trials for the treatment of multiple subtypes of breast cancer, prostate cancer and a Phase II trial for haematologic malignancies.


Lead Product(s): Capivasertib,Fulvestrant

Therapeutic Area: Oncology Brand Name: AZD 5363

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 08, 2022

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10

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

AstraZeneca

United Kingdom
arrow
Medlab Asia & Asia Health
Not Confirmed

Details : Capivasertib (AZD 5363), is an investigational oral treatment currently in Phase III trials for the treatment of multiple subtypes of breast cancer, prostate cancer and a Phase II trial for haematologic malignancies.

Brand Name : AZD 5363

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 08, 2022

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