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Chemistry

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Also known as: Abl-001, 1492952-76-7, Abl001, Asciminib free base, Abl001-nx, Nvp-abl001
Molecular Formula
C20H18ClF2N5O3
Molecular Weight
449.8  g/mol
InChI Key
VOVZXURTCKPRDQ-CQSZACIVSA-N
FDA UNII
L1F3R18W77

Asciminib
Asciminib is an orally bioavailable, allosteric Bcr-Abl1 tyrosine kinase inhibitor, with antineoplastic activity. Upon administration, asciminib targets and binds to the myristoyl pocket of the Bcr-Abl1 fusion protein at a location that is distinct from the ATP-binding domain, thereby inhibiting the activity of both wild-type Bcr-Abl and certain mutation forms, including the T315I mutation. This binding results in the inhibition of Bcr-Abl1-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies. The Bcr-Abl1 fusion protein tyrosine kinase is an abnormal enzyme produced by leukemia cells that contain the Philadelphia chromosome.
1 2D Structure

Asciminib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-[4-[chloro(difluoro)methoxy]phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide
2.1.2 InChI
InChI=1S/C20H18ClF2N5O3/c21-20(22,23)31-15-3-1-13(2-4-15)26-19(30)12-9-16(17-5-7-25-27-17)18(24-10-12)28-8-6-14(29)11-28/h1-5,7,9-10,14,29H,6,8,11H2,(H,25,27)(H,26,30)/t14-/m1/s1
2.1.3 InChI Key
VOVZXURTCKPRDQ-CQSZACIVSA-N
2.1.4 Canonical SMILES
C1CN(CC1O)C2=C(C=C(C=N2)C(=O)NC3=CC=C(C=C3)OC(F)(F)Cl)C4=CC=NN4
2.1.5 Isomeric SMILES
C1CN(C[C@@H]1O)C2=C(C=C(C=N2)C(=O)NC3=CC=C(C=C3)OC(F)(F)Cl)C4=CC=NN4
2.2 Other Identifiers
2.2.1 UNII
L1F3R18W77
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Abl001

2. Asciminib Hydrochloride

2.3.2 Depositor-Supplied Synonyms

1. Abl-001

2. 1492952-76-7

3. Abl001

4. Asciminib Free Base

5. Abl001-nx

6. Nvp-abl001

7. Asciminib [usan]

8. Scemblix

9. Example 9

10. L1f3r18w77

11. 1492952-76-7 (free Base)

12. (r)-n-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1h-pyrazol-5-yl)nicotinamide

13. 3-pyridinecarboxamide, N-(4-(chlorodifluoromethoxy)phenyl)-6-((3r)-3-hydroxy-1-pyrrolidinyl)-5-(1h-pyrazol-3-yl)-

14. N-[4-[chloro(difluoro)methoxy]phenyl]-6-[(3r)-3-hydroxypyrrolidin-1-yl]-5-(1h-pyrazol-5-yl)pyridine-3-carboxamide

15. 3-pyridinecarboxamide, N-[4-(chlorodifluoromethoxy)phenyl]-6-[(3r)-3-hydroxy-1-pyrrolidinyl]-5-(1h-pyrazol-3-yl)-

16. Asciminib [inn]

17. Asciminib (abl001)

18. Asciminib (usan/inn)

19. Asciminib [who-dd]

20. Unii-l1f3r18w77

21. Gtpl8962

22. Chembl4208229

23. Schembl15388306

24. Tqp0925

25. Ex-a3030

26. Bdbm50459091

27. Nsc789925

28. S8555

29. Zinc150275965

30. At30330

31. Ccg-269232

32. Compound 1 [pmid: 30137981]

33. Cs-7655

34. Db12597

35. Nsc-789925

36. (r)-n- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- Hydroxypyrrolidin-1- Yl)-5- (1h-pyrazol- 5-yl)nicotinamide

37. Ba166957

38. Bs-15538

39. Hy-104010

40. D11403

41. A910986

42. Q27074535

43. (r)-n-(4-(chloro Difluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1h-pyrazol-5-yl)nicotinamide

44. (r)-n-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1h-pyrazol-3-yl)nicotinamide

45. Ay7

46. N-(4-(chlorodifluoromethoxy)phenyl)-6-((3r)-3- Hydroxypyrrolidin-1-yl)-5-(1h-pyrazol-3-yl)pyridine- 3-carboxamide

2.4 Create Date
2013-12-02
3 Chemical and Physical Properties
Molecular Weight 449.8 g/mol
Molecular Formula C20H18ClF2N5O3
XLogP33
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count8
Rotatable Bond Count6
Exact Mass449.1066235 g/mol
Monoisotopic Mass449.1066235 g/mol
Topological Polar Surface Area103 Ų
Heavy Atom Count31
Formal Charge0
Complexity626
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

Asciminib is indicated for the treatment of adult patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase who have been previously treated with 2 tyrosine kinase inhibitors. It is also indicated in the treatment of Ph+ CML in adult patients with the T315I mutation.


Scemblix is indicated for the treatment of adult patients with Philadelphia chromosome positive chronic myeloid leukaemia in chronic phase (Ph+ CML CP) previously treated with two or more tyrosine kinase inhibitors (see section 5. 1).


5 Pharmacology and Biochemistry
5.1 Pharmacology

Asciminib exerts its therapeutic activity by inhibiting an oncogenic protein responsible for the proliferation of CML. It may be administered orally once or twice a day depending on the condition being treated. By increasing the total daily dose 5-fold as compared to standard therapy (80mg daily vs. 400mg daily), it can be used to treat Ph+ CML with the T315I mutation, a typically treatment-resistant variant of the disease. As with many other chemotherapeutic agents, asciminib treatment can result in various forms of myelosuppression, including thrombocytopenia and neutropenia. Patients should receive frequent laboratory monitoring throughout therapy and dose adjustments may be required based on the severity of observed effects. Patients may also experience pancreatic and/or cardiovascular toxicity, both of which require frequent monitoring and may require dose adjustments as per prescribing information.


5.2 ATC Code

L01EA06


L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EA - Bcr-abl tyrosine kinase inhibitors

L01EA06 - Asciminib


5.3 Absorption, Distribution and Excretion

Absorption

The median Tmax of asciminib following oral administration is 2.5 hours. At a dose of 80mg once daily, the steady-state Cmax and AUCtau were 1781 ng/mL and 15112 ng.h/mL, respectively. At a dose of 40mg twice daily, the steady-state Cmax and AUCtau were 793 ng/mL and 5262 ng.h/mL, respectively. At a dose of 200mg twice daily (for treatment of T315I mutants), the steady-state Cmax and AUCtau were 5642 ng/mL and 37547 ng.h/mL, respectively. As compared to the fasted state, the co-administration of asciminib with a high-fat meal decreased the AUC and Cmax by 62% and 68%, respectively, and its co-administration with a low-fat meal decreased the AUC and Cmax by 30% and 35%, respectively.


Route of Elimination

Asciminib is eliminated via biliary secretion facilitated by breast cancer-resistant protein (BCRP) transporters. Following oral administration, approximately 80% and 11% of an asciminib dose was recovered in the feces and urine, respectively. Unchanged parent drug accounted for 57% of drug material recovered in the feces and 2.5% in the urine.


Volume of Distribution

At steady-state, the apparent volume of distribution of asciminib is 151 L.


Clearance

The total apparent clearance of asciminib is 6.7 L/h at a total daily dose of 80mg and 4.1 L/h at a dose of 200mg twice daily.


5.4 Metabolism/Metabolites

Asciminib is negligibly metabolized, with unchanged parent drug comprising the main drug component in plasma (~93%) and following excretion (~57% in feces). The main circulating metabolites are M30.5, M44, and M29.5, accounting for approximately 5%, 2%, and 0.4% of the total administered dose, respectively. The oxidative metabolism of asciminib is mediated by CYP3A4, and the glucuronidation of asciminib is mediated by UGT2B7 and UGT2B17.


5.5 Biological Half-Life

The terminal elimination half-life asciminib is 5.5 hours when administered at 40mg twice daily and 9.0 hours when administered at 200mg twice daily.


5.6 Mechanism of Action

In most patients with chronic myeloid leukemia (CML), progression of the disease is driven primarily by a translocation of the Philadelphia chromosome that creates an oncogenic fusion gene, _BCR-ABL1_, between the _BCR_ and _ABL1_ genes. This fusion gene produces a resultant fusion protein, BCR-ABL1, which exhibits elevated tyrosine kinase and transforming activities that contribute to CML proliferation. Asciminib is an allosteric inhibitor of the BCR-ABL1 tyrosine kinase. It binds to the myristoyl pocket of the ABL1 portion of the fusion protein and locks it into an inactive conformation, preventing its oncogenic activity.


Drugs in Development

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Details:

Scemblix (asciminib) works by specifically targeting Bcr/Abl fusion protein. It is being evaluated for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia.


Lead Product(s): Asciminib

Therapeutic Area: Oncology Brand Name: Scemblix

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 31, 2024

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01

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : Scemblix (asciminib) works by specifically targeting Bcr/Abl fusion protein. It is being evaluated for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia.

Brand Name : Scemblix

Molecule Type : Small molecule

Upfront Cash : Not Applicable

May 31, 2024

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Details:

Scemblix (asciminib) works by specifically targeting the ABL myristoyl pocket & acts as Bcr/Abl fusion protein inhibitor. It is being evaluated for the treatment of chronic myeloid leukemia.


Lead Product(s): Asciminib

Therapeutic Area: Oncology Brand Name: Scemblix

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable January 08, 2024

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02

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : Scemblix (asciminib) works by specifically targeting the ABL myristoyl pocket & acts as Bcr/Abl fusion protein inhibitor. It is being evaluated for the treatment of chronic myeloid leukemia.

Brand Name : Scemblix

Molecule Type : Small molecule

Upfront Cash : Not Applicable

January 08, 2024

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Details:

Approval based on trial, in which Scemblix® (asciminib) nearly doubled major molecular response rate vs. Bosulif®* (bosutinib) (25.5% vs. 13.2%) with more than three times lower discontinuation rate due to adverse reactions at 24 weeks and confirmed at 96 weeks.


Lead Product(s): Asciminib

Therapeutic Area: Oncology Brand Name: Scemblix

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable August 29, 2022

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03

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : Approval based on trial, in which Scemblix® (asciminib) nearly doubled major molecular response rate vs. Bosulif®* (bosutinib) (25.5% vs. 13.2%) with more than three times lower discontinuation rate due to adverse reactions at 24 weeks and confirmed at...

Brand Name : Scemblix

Molecule Type : Small molecule

Upfront Cash : Not Applicable

August 29, 2022

blank

Details:

Positive opinion based on data showed near doubling in major molecular response rate for patients treated with Scemblix® (asciminib) vs. Bosulif (bosutinib) and more than 3 times lower discontinuation rate due to adverse reactions at 24 weeks.


Lead Product(s): Asciminib

Therapeutic Area: Oncology Brand Name: Scemblix

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 24, 2022

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04

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : Positive opinion based on data showed near doubling in major molecular response rate for patients treated with Scemblix® (asciminib) vs. Bosulif (bosutinib) and more than 3 times lower discontinuation rate due to adverse reactions at 24 weeks.

Brand Name : Scemblix

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 24, 2022

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Details:

Scemblix® (asciminib) continues to show superior efficacy with more-than-two-fold improvement in major molecular response rate vs. Bosulif®* (bosutinib) at 96 weeks (37.6% vs. 15.8%), building on 24-week results.


Lead Product(s): Asciminib

Therapeutic Area: Oncology Brand Name: Scemblix

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 07, 2022

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05

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : Scemblix® (asciminib) continues to show superior efficacy with more-than-two-fold improvement in major molecular response rate vs. Bosulif®* (bosutinib) at 96 weeks (37.6% vs. 15.8%), building on 24-week results.

Brand Name : Scemblix

Molecule Type : Small molecule

Upfront Cash : Not Applicable

June 07, 2022

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Details:

ES104 (asciminib) demonstrated, 42% overall response rate (ORR) based on 10 patients with Partial Responses (PRs), including 9 PRs confirmed by RECIST 1.1 and 1 PR pending confirmation.


Lead Product(s): Asciminib,Paclitaxel

Therapeutic Area: Oncology Brand Name: ES104

Study Phase: Phase I/ Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 05, 2022

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06

Elpiscience

China
arrow
Skin Aging & Challenges
Not Confirmed

Elpiscience

China
arrow
Skin Aging & Challenges
Not Confirmed

Details : ES104 (asciminib) demonstrated, 42% overall response rate (ORR) based on 10 patients with Partial Responses (PRs), including 9 PRs confirmed by RECIST 1.1 and 1 PR pending confirmation.

Brand Name : ES104

Molecule Type : Small molecule

Upfront Cash : Not Applicable

May 05, 2022

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Details:

CTX-009 (asciminib), a bispecific antibody demonstrated a 42% overall response rate (ORR) based on 10 patients with Partial Responses (PRs), including 9 PRs confirmed by RECIST 1.1 and 1 PR pending confirmation.


Lead Product(s): Asciminib,Paclitaxel

Therapeutic Area: Oncology Brand Name: CTX-009

Study Phase: Phase I/ Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 04, 2022

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07

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : CTX-009 (asciminib), a bispecific antibody demonstrated a 42% overall response rate (ORR) based on 10 patients with Partial Responses (PRs), including 9 PRs confirmed by RECIST 1.1 and 1 PR pending confirmation.

Brand Name : CTX-009

Molecule Type : Small molecule

Upfront Cash : Not Applicable

May 04, 2022

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Details:

CTX-009 (asciminib) is a bispecific antibody that simultaneously targets Delta-like ligand 4 (DLL4) and vascular endothelial growth factor A (VEGF-A), also has demonstrated clinical benefit in heavily pre-treated patients who have progressed after prior targeted therapies.


Lead Product(s): Asciminib,Paclitaxel

Therapeutic Area: Oncology Brand Name: CTX-009

Study Phase: Phase I/ Phase IIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 03, 2022

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08

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : CTX-009 (asciminib) is a bispecific antibody that simultaneously targets Delta-like ligand 4 (DLL4) and vascular endothelial growth factor A (VEGF-A), also has demonstrated clinical benefit in heavily pre-treated patients who have progressed after prior ...

Brand Name : CTX-009

Molecule Type : Small molecule

Upfront Cash : Not Applicable

May 03, 2022

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Details:

New longer-term efficacy and safety data from pivotal Phase III ASCEMBL study for recently US-approved Scemblix® (asciminib) in patients with PH+ CML-CP.


Lead Product(s): Asciminib

Therapeutic Area: Oncology Brand Name: Scemblix

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 04, 2021

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09

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : New longer-term efficacy and safety data from pivotal Phase III ASCEMBL study for recently US-approved Scemblix® (asciminib) in patients with PH+ CML-CP.

Brand Name : Scemblix

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 04, 2021

blank

Details:

SCEMBLIX® (asciminib) tablets is a prescription medicine used to treat adults with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP), previously treated with 2 or more tyrosine kinase inhibitor (TKI) medicines.


Lead Product(s): Asciminib

Therapeutic Area: Oncology Brand Name: Scemblix

Study Phase: ApprovedProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 29, 2021

blank

10

Skin Aging & Challenges
Not Confirmed
Skin Aging & Challenges
Not Confirmed

Details : SCEMBLIX® (asciminib) tablets is a prescription medicine used to treat adults with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP), previously treated with 2 or more tyrosine kinase inhibitor (TKI) medicines.

Brand Name : Scemblix

Molecule Type : Small molecule

Upfront Cash : Not Applicable

October 29, 2021

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Patents & EXCLUSIVITIES

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US Patents

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NOVARTIS

Switzerland
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ASCIMINIB HYDROCHLORIDE

US Patent Number : 11407735

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 215358

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2040-05-14

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NOVARTIS

Switzerland
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2024 ACI Convention
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ASCIMINIB HYDROCHLORIDE

US Patent Number : 8829195

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 215358

Patent Use Code : U-1374

Delist Requested :

Patent Use Description : TREATMENT OF PHILADELP...

Patent Expiration Date : 2033-05-13

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2024 ACI Convention
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NOVARTIS

Switzerland
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2024 ACI Convention
Not Confirmed

ASCIMINIB HYDROCHLORIDE

US Patent Number : 8829195

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 215358

Patent Use Code : U-1374

Delist Requested :

Patent Use Description : TREATMENT OF PHILADELP...

Patent Expiration Date : 2033-05-13

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04

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2024 ACI Convention
Not Confirmed

NOVARTIS

Switzerland
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2024 ACI Convention
Not Confirmed

ASCIMINIB HYDROCHLORIDE

US Patent Number : 8829195

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 215358

Patent Use Code : U-1374

Delist Requested :

Patent Use Description : TREATMENT OF PHILADELP...

Patent Expiration Date : 2033-05-13

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05

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2024 ACI Convention
Not Confirmed

NOVARTIS

Switzerland
arrow
2024 ACI Convention
Not Confirmed

ASCIMINIB HYDROCHLORIDE

US Patent Number : 11407735

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 215358

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2040-05-14

blank

06

arrow
2024 ACI Convention
Not Confirmed

NOVARTIS

Switzerland
arrow
2024 ACI Convention
Not Confirmed

ASCIMINIB HYDROCHLORIDE

US Patent Number : 11407735

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 215358

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2040-05-14

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