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Synopsis

ACTIVE PHARMA INGREDIENTS

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0INTERMEDIATES

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Chemistry

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Also known as: 1353550-13-6, Hm61713, Bi 1482694, 1802181-20-9, Olmutinib [inn], Hm-61713
Molecular Formula
C26H26N6O2S
Molecular Weight
486.6  g/mol
InChI Key
FDMQDKQUTRLUBU-UHFFFAOYSA-N
FDA UNII
CHL9B67L95

Olmutinib
Olmutinib is an orally available small molecule, mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit the EGFR wild type form.
1 2D Structure

Olmutinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-[3-[2-[4-(4-methylpiperazin-1-yl)anilino]thieno[3,2-d]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
2.1.2 InChI
InChI=1S/C26H26N6O2S/c1-3-23(33)27-19-5-4-6-21(17-19)34-25-24-22(11-16-35-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h3-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)
2.1.3 InChI Key
FDMQDKQUTRLUBU-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)SC=C4
2.2 Other Identifiers
2.2.1 UNII
CHL9B67L95
2.3 Synonyms
2.3.1 Depositor-Supplied Synonyms

1. 1353550-13-6

2. Hm61713

3. Bi 1482694

4. 1802181-20-9

5. Olmutinib [inn]

6. Hm-61713

7. Olmutinib [who-dd]

8. Bi-1482694

9. N-[3-[2-[4-(4-methylpiperazin-1-yl)anilino]thieno[3,2-d]pyrimidin-4-yl]oxyphenyl]prop-2-enamide

10. Chl9b67l95

11. N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)thieno[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide

12. N-{3-[(2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}thieno[3,2-d]pyrimidin-4-yl)oxy]phenyl}prop-2-enamide

13. 2-propenamide, N-(3-((2-((4-(4-methyl-1-piperazinyl)phenyl)amino)thieno(3,2-d)pyrimidin-4-yl)oxy)phenyl)-

14. N-(3-((2-(4-(4-methylpiperazin-1-yl)anilino)thieno(3,2-d)pyrimidin-4-yl)oxy)phenyl)prop-2-enamide

15. 1938072-69-5

16. 2-propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]-

17. Hm-61713 (bi-1482694)

18. Hm 61713

19. Hm71224;olmutinib

20. Olmutinib (usan/inn)

21. Olmutinib [usan:inn]

22. Olmutinib [usan]

23. Olmutinib(hm-71224)

24. Unii-chl9b67l95

25. Gtpl9196

26. Chembl3786343

27. Schembl14914931

28. Ex-a879

29. Dtxsid001319119

30. Bcp16733

31. Bdbm50160871

32. Mfcd29918158

33. Nsc792848

34. Nsc800980

35. S8294

36. Akos030632791

37. Zinc198970879

38. Ccg-269594

39. Cs-5413

40. Db13164

41. Nsc-792848

42. Nsc-800980

43. Sb19797

44. Example 1 [us20130116213]

45. Ac-30225

46. Ac-35418

47. As-74850

48. Hm 71224

49. Hy-19730

50. Bi1482694

51. Ds-015877

52. Ft-0700176

53. Olmutinib (hm61713, Bi 1482694)

54. J3.435.413h

55. D10859

56. W12116

57. Hm61713, Bi 1482694

58. A900418

59. J-690142

60. Q27088175

61. 4-{[4-({[(1r,2s)-2-phenylcyclopropyl]amino}methyl)-1-piperidinyl]methyl}benzoic Acid

62. Bi1482694;bi 1482694;bi-1482694;hm 61713;hm-61713;hm61713

63. N-(3-(2-(4-(4 Methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidine-4-yloxy)phenyl)acrylamide

64. N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidine-4-yloxy)phenyl)acrylamide

65. N-(3-{2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-thieno[3,2-d]pyrimidin-4-yloxy}-phenyl)-acrylamide

2.4 Create Date
2012-01-09
3 Chemical and Physical Properties
Molecular Weight 486.6 g/mol
Molecular Formula C26H26N6O2S
XLogP34.7
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count8
Rotatable Bond Count7
Exact Mass486.18379527 g/mol
Monoisotopic Mass486.18379527 g/mol
Topological Polar Surface Area111 Ų
Heavy Atom Count35
Formal Charge0
Complexity712
Isotope Atom Count0
Defined Atom Stereocenter Count0
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

For use in treatment of metastatic T790M mutation positive non-small cell lung cancer.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Olmutinib selectively and irreversibly binds and inhibits epidermal growth factor receptors (EGFR) with the T790M activating mutation. EGFRs are frequently over-expressed in lung cancer and contribute to activation of the phosphoinositide 3-kinase and mitogen activated protein kinase pathways which both promote cell survival and proliferation. By inhibiting EGFR activation, olmutinib attenuates the activation of these tumor promoting pathways.


5.2 ATC Code

L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EB - Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors

L01EB06 - Olmutinib


5.3 Absorption, Distribution and Excretion

Absorption

tmax of 3-4h with oral administration.


Route of Elimination

Data not yet available.


Volume of Distribution

Data not yet available.


Clearance

Data not yet available.


5.4 Metabolism/Metabolites

Data not yet available.


5.5 Biological Half-Life

8-11h.


5.6 Mechanism of Action

Olmutinib covalently binds a cysteine residue near the kinase domain of mutant EGFRs to prevent phosphorylation of the receptor. This inhibits receptor signalling as phosphorylation is necessary for recruitment of signalling cascade proteins.


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Looking for 1353550-13-6 / Olmutinib API manufacturers, exporters & distributors?

Olmutinib manufacturers, exporters & distributors 1

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

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Olmutinib manufacturer or Olmutinib supplier.

PharmaCompass also assists you with knowing the Olmutinib API Price utilized in the formulation of products. Olmutinib API Price is not always fixed or binding as the Olmutinib Price is obtained through a variety of data sources. The Olmutinib Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

Olmutinib

Synonyms

1353550-13-6, Hm61713, Bi 1482694, 1802181-20-9, Olmutinib [inn], Hm-61713

Cas Number

1353550-13-6

Unique Ingredient Identifier (UNII)

CHL9B67L95

About Olmutinib

Olmutinib is an orally available small molecule, mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit the EGFR wild type form.

Olmutinib Manufacturers

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

Olmutinib Suppliers

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

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

Olmutinib KDMF

In Korea, the Ministry of Food and Drug Safety (MFDS) is in charge of regulating pharmaceutical products and services.

Pharmaceutical companies submit a Olmutinib Drug Master File in Korea (Olmutinib KDMF) to the MFDS, which includes comprehensive information about the production, processing, facilities, materials, packaging, and testing of Olmutinib. The MFDS reviews the Olmutinib KDMF as part of the drug registration process and uses the information provided in the Olmutinib KDMF to evaluate the safety and efficacy of the drug.

After submitting a Olmutinib KDMF to the MFDS, the registered manufacturer can provide importers or distributors with the registration number without revealing confidential information to Korean business partners. Applicants seeking to register their Olmutinib API can apply through the Korea Drug Master File (KDMF).

click here to find a list of Olmutinib suppliers with KDMF on PharmaCompass.

Olmutinib GMP

Olmutinib 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 Olmutinib 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 Olmutinib GMP manufacturer or Olmutinib GMP API supplier for your needs.

Olmutinib CoA

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

Olmutinib CoA mostly includes findings from lab analyses of a specific batch. For each Olmutinib 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.

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