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Pralsetinib

Pralsetinib

Synopsis, Chemistry

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Also known as: Blu-667, 2097132-94-8, Pralsetinib free base, Gavreto, Cis-pralsetinib, Blu667

Molecular Formula

C₂₇H₃₂FN₉O₂

Molecular Weight

533.6 g/mol

InChI Key

GBLBJPZSROAGMF-SIYOEGHHSA-N

FDA UNII

1WPE73O1WV

Pralsetinib is an orally bioavailable selective inhibitor of mutant forms of and fusion products involving the proto-oncogene receptor tyrosine kinase RET, with potential antineoplastic activity. Upon administration, pralsetinib binds to and targets various RET mutants and RET-containing fusion product. RET gene mutations and translocations result in the upregulation and/or activation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and regression of these cancers.

Pralsetinib is a Kinase Inhibitor. The mechanism of action of pralsetinib is as a Rearranged during Transfection (RET) Inhibitor.

1 2D Structure

Pralsetinib

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

N-[(1S)-1-[6-(4-fluoropyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide

2.1.2 InChI

InChI=1S/C27H32FN9O2/c1-16-11-22(33-23-12-17(2)35-36-23)34-25(31-16)19-7-9-27(39-4,10-8-19)26(38)32-18(3)20-5-6-24(29-13-20)37-15-21(28)14-30-37/h5-6,11-15,18-19H,7-10H2,1-4H3,(H,32,38)(H2,31,33,34,35,36)/t18-,19?,27?/m0/s1

2.1.3 InChI Key

GBLBJPZSROAGMF-SIYOEGHHSA-N

2.1.4 Canonical SMILES

CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)NC(C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC

2.1.5 Isomeric SMILES

CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)N[C@@H](C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC

2.2 Other Identifiers

2.2.1 UNII

1WPE73O1WV

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Blu-667

2. Cyclohexanecarboxamide, N-((1s)-1-(6-(4-fluoro-1h-pyrazol-1-yl)-3-pyridinyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1h-pyrazol-3-yl)amino)-2-pyrimidinyl)-, Trans-

3. Gavreto

4. Trans-n-((1s)-1-(6-(4-fluoro-1h-pyrazol-1-yl)-3-pyridinyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1h-pyrazol-3-yl)amino)-2-pyrimidinyl)cyclohexanecarboxamide

2.3.2 Depositor-Supplied Synonyms

1. Blu-667

2. 2097132-94-8

3. Pralsetinib Free Base

4. Gavreto

5. Cis-pralsetinib

6. Blu667

7. Trans-pralsetinib

8. Pralsetinib [inn]

9. Pralsetinib [usan]

10. Blu123244

11. 1wpe73o1wv

12. 2097132-93-7

13. X581238

14. 2097132-94-8 (free Base)

15. Blu-123244

16. N-[(1s)-1-[6-(4-fluoropyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide

17. X-581238

18. (cis)-n-((s)-1-(6-(4-fluoro-1h-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-(5-methyl-1h-pyrazol-3-ylamino)pyrimidin-2-yl)cyclohexanecarboxamide

19. Cis-n-{(1s)-1-[6-(4-fluoro-1h-pyrazol-1-yl)pyridin-3-yl]ethyl}-1-methoxy-4-{4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide

20. Cyclohexanecarboxamide, N-((1s)-1-(6-(4-fluoro-1h-pyrazol-1-yl)-3-pyridinyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1h-pyrazol-3-yl)amino)-2-pyrimidinyl)-, Cis-

21. Cyclohexanecarboxamide, N-[(1s)-1-[6-(4-fluoro-1h-pyrazol-1-yl)-3-pyridinyl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]-2-pyrimidinyl]-, Cis-

22. Q4j

23. Blu667blu667

24. Cis-blu-667

25. Pralsetinib (usan/inn)

26. Blu-667 (pralsetinib)

27. Unii-1wpe73o1wv

28. Pralsetinib [who-dd]

29. Chembl4582651

30. Schembl18789228

31. Schembl18789229

32. Schembl18806610

33. Gtpl10033

34. Bdbm435009

35. Bdbm435010

36. Dtxsid901336540

37. Amy16875

38. Ex-a1944

39. Ex-a3347

40. Nsc811429

41. S8716

42. Us10584114, Compound 129

43. Us10584114, Compound 130

44. Who 11004

45. Akos037648884

46. Hy-112301a

47. Nsc-811429

48. Ac-35657

49. Bs-15942

50. Hy-112301

51. Cs-0043448

52. Cs-0044766

53. D11712

54. Blu-667; Trans-n-{(1s)-1-[6-(4-fluoro-1h-pyrazol-1-yl)pyridin-3-yl]ethyl}-1-methoxy-4-{4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide

55. Trans-n-{(1s)-1-[6-(4-fluoro-1h-pyrazol-1-yl)pyridin-3-yl]ethyl}-1-methoxy-4-{4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide

2.4 Create Date

2017-08-04

3 Chemical and Physical Properties

Molecular Formula	C₂₇H₃₂FN₉O₂
Molecular Weight	533.6 g/mol
XLogP3	3.1
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	8
Exact Mass	533.26629946 g/mol
Monoisotopic Mass	533.26629946 g/mol
Topological Polar Surface Area	136 Å²
Heavy Atom Count	39
Formal Charge	0
Complexity	816
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

4 Drug and Medication Information

4.1 Drug Indication

Treatment of lung cancer (small cell and non-small cell lung cancer )

Gavreto is indicated as monotherapy for the treatment of adult patients with rearranged during transfection (RET) fusion-positive advanced non-small cell lung cancer (NSCLC) not previously treated with a RET inhibitor.

Treatment of thyroid cancer

5 Pharmacology and Biochemistry

5.1 MeSH Pharmacological Classification

Antineoplastic Agents

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

PRALSETINIB

5.2.2 FDA UNII

1WPE73O1WV

5.2.3 Pharmacological Classes

Rearranged during Transfection (RET) Inhibitors [MoA]; Kinase Inhibitor [EPC]