Find Acalabrutinib manufacturers, exporters & distributors on PharmaCompass

PharmaCompass

Synopsis

Synopsis

API REF. PRICE (USD/KG)

MARKET PLACE

0

API

0

FDF

FDF Dossiers

DRUG PRODUCT COMPOSITIONS

REF. STANDARDS OR IMPURITIES

0

EDQM

0

USP

0

JP

0

Others

PATENTS & EXCLUSIVITIES

0

Health Canada Patents

DIGITAL CONTENT

0

Stock Recap #PipelineProspector

0

Weekly News Recap #Phispers

97 RELATED EXCIPIENT COMPANIES

163EXCIPIENTS BY APPLICATIONS

Chemistry

Click the arrow to open the dropdown
read-moreClick the button for full data set
Also known as: 1420477-60-6, Acp-196, Calquence, Acalabrutinib (acp-196), Acalabrutinib [inn], I42748elqw
Molecular Formula
C26H23N7O2
Molecular Weight
465.5  g/mol
InChI Key
WDENQIQQYWYTPO-IBGZPJMESA-N
FDA UNII
I42748ELQW

Acalabrutinib
Acalabrutinib is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, acalabrutinib inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.
Acalabrutinib is a Kinase Inhibitor. The mechanism of action of acalabrutinib is as a Tyrosine Kinase Inhibitor.
1 2D Structure

Acalabrutinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
4-[8-amino-3-[(2S)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-pyridin-2-ylbenzamide
2.1.2 InChI
InChI=1S/C26H23N7O2/c1-2-6-21(34)32-15-5-7-19(32)25-31-22(23-24(27)29-14-16-33(23)25)17-9-11-18(12-10-17)26(35)30-20-8-3-4-13-28-20/h3-4,8-14,16,19H,5,7,15H2,1H3,(H2,27,29)(H,28,30,35)/t19-/m0/s1
2.1.3 InChI Key
WDENQIQQYWYTPO-IBGZPJMESA-N
2.1.4 Canonical SMILES
CC#CC(=O)N1CCCC1C2=NC(=C3N2C=CN=C3N)C4=CC=C(C=C4)C(=O)NC5=CC=CC=N5
2.1.5 Isomeric SMILES
CC#CC(=O)N1CCC[C@H]1C2=NC(=C3N2C=CN=C3N)C4=CC=C(C=C4)C(=O)NC5=CC=CC=N5
2.2 Other Identifiers
2.2.1 UNII
I42748ELQW
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Acp-196

2. Calquence

2.3.2 Depositor-Supplied Synonyms

1. 1420477-60-6

2. Acp-196

3. Calquence

4. Acalabrutinib (acp-196)

5. Acalabrutinib [inn]

6. I42748elqw

7. 4-[8-amino-3-[(2s)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-n-pyridin-2-ylbenzamide

8. Benzamide, 4-(8-amino-3-((2s)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl)imidazo(1,5-a)pyrazin-1-yl)-n-2-pyridinyl-

9. (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamide

10. Acalabrutinib(acp196)

11. Acalabrutinib [usan:inn]

12. Acalabrutinibum

13. Unii-i42748elqw

14. Calquence (tn)

15. Benzamide, 4-[8-amino-3-[(2s)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl]-n-2-pyridinyl-

16. Acp-196;acalabrutinib

17. Acalabrutinib [mi]

18. Acalabrutinib [jan]

19. Acalabrutinib [usan]

20. Acalabrutinib [who-dd]

21. Gtpl8912

22. Acalabrutinib (jan/usan/inn)

23. Chembl3707348

24. Schembl14637368

25. Acp 196

26. Amy5290

27. Ex-a881

28. Chebi:167707

29. Dtxsid401026209

30. Acalabrutinib [orange Book]

31. Bdbm50175583

32. Mfcd29472294

33. Nsc791164

34. Nsc800976

35. S8116

36. Zinc208774715

37. Ccg-269407

38. Cs-5356

39. Db11703

40. Ds-3326

41. Nsc-791164

42. Nsc-800976

43. Ncgc00479074-01

44. Hy-17600

45. Example 6 [us20140155385 A1]

46. D10893

47. A857446

48. J-690166

49. Q23668732

50. (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamide;acalabrutinib

51. (s)-4-(8-amino-3-(1-but-2-ynoylpyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamide

52. 4-[8-amino-3-[(2s)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl]-n-2-pyridinyl-benzamide

53. 4-[8-amino-3-[(2s)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-n-(2-pyridyl)benzamide

54. 4-{8-amino-3-[(2s)-1-(but-2-ynoyl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-n-(pyridin-2-yl)benzamide

2.4 Create Date
2013-03-21
3 Chemical and Physical Properties
Molecular Weight 465.5 g/mol
Molecular Formula C26H23N7O2
XLogP33
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count6
Rotatable Bond Count4
Exact Mass465.19132300 g/mol
Monoisotopic Mass465.19132300 g/mol
Topological Polar Surface Area119 Ų
Heavy Atom Count35
Formal Charge0
Complexity845
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 Information
1 of 1  
Drug NameCALQUENCE
Active IngredientACALABRUTINIB
CompanyASTRAZENECA (Application Number: N210259. Patents: 9290504, 9758524, 9796721)

4.2 Drug Indication

Acalabrutinib is currently indicated for the treatment of adult patients with Mantle Cell Lymphoma (MCL) who have received at least one prior therapy. It has also been recently approved for chronic lymphocytic leukemia and small lymphocytic lymphoma.


FDA Label


Calquence as monotherapy or in combination with obinutuzumab is indicated for the treatment of adult patients with previously untreated chronic lymphocytic leukaemia (CLL).

Calquence as monotherapy is indicated for the treatment of adult patients with chronic lymphocytic leukaemia (CLL) who have received at least one prior therapy.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Acalabrutinib is a Bruton Tyrosine Kinase inhibitor that prevents the proliferation, trafficking, chemotaxis, and adhesion of B cells. It is taken every 12 hours and can cause other effects such as atrial fibrillation, other malignancies, cytopenia, hemorrhage, and infection.


5.2 MeSH Pharmacological Classification

Antineoplastic Agents

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


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
ACALABRUTINIB
5.3.2 FDA UNII
I42748ELQW
5.3.3 Pharmacological Classes
Tyrosine Kinase Inhibitors [MoA]; Kinase Inhibitor [EPC]
5.4 ATC Code

L01XE51


L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EL - Bruton's tyrosine kinase (btk) inhibitors

L01EL02 - Acalabrutinib


5.5 Absorption, Distribution and Excretion

Absorption

The geometric mean absolute bioavailability of acalabrutinib is 25% with a median time to peak plasma concentrations (Tmax) of 0.75 hours.


Route of Elimination

After administration of a single 100 mg radiolabelled acalabrutinib dose in healthy subjects, 84% of the dose was recovered in the feces and 12% of the dose was recovered in the urine. An irradiated dose of acalabrutinib was 34.7% recovered as the metabolite ACP-5862; 8.6% was recovered as unchanged acalabrutinub; 10.8 was recovered as a mixture of the M7, M8, M9, M10, and M11 metabolites; 5.9% was the M25 metabolite; 2.5% was recovered as the M3 metabolite.


Volume of Distribution

The mean steady-state volume of distribution is approximately 34 L.


Clearance

Acalabrutinib's mean apparent oral clearance (CL/F) is observed to be 159 L/hr with similar PK between patients and healthy subjects, based on population PK analysis.


5.6 Metabolism/Metabolites

Acalabrutinib is mainly metabolized by CYP3A enzymes. ACP-5862 is identified to be the major active metabolite in plasma with a geometric mean exposure (AUC) that is about 2-3 times greater than the exposure of acalabrutinib. ACP-5862 is about 50% less potent than acalabrutinib in regards to the inhibition of BTK.


5.7 Biological Half-Life

After administering a single oral dose of 100 mg acalabrutinib, the median terminal elimination half-life of the drug was found to be 0.9 (with a range of 0.6 to 2.8) hours. The half-life of the active metabolite, ACP-5862, is about 6.9 hours.


5.8 Mechanism of Action

Mantle Cell Lymphoma (MCL) is a rare yet aggressive type of B-cell non-Hodgkin lymphoma (NHL) with poor prognosis. Subsequently, relapse is common in MCL patients and ultimately represents disease progression. Lymphoma occurs when immune system lymphocytes grow and multiply uncontrollably. Such cancerous lymphocytes may travel to many parts of the body, including the lymph nodes, spleen, bone marrow, blood, and other organs where they can multiply and form a mass(es) called a tumor. One of the main kinds of lymphocytes that can develop into cancerous lymphomas are the body's own B-lymphocytes (B-cells). Bruton Tyrosine Kinase (BTK) is a signalling molecule of the B-cell antigen receptor and cytokine receptor pathways. Such BTK signaling causes the activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion. Acalabrutinib is a small molecule inhibitor of BTK. Both acalabrutinib and its active metabolite, ACP-5862, act to form a covalent bond with a cysteine residue (Cys481) in the BTK active site, leading to inhibition of BTK enzymatic activity. As a result, acalabrutinib inhibits BTK-mediated activation of downstream signaling proteins CD86 and CD69, which ultimately inhibits malignant B-cell proliferation and survival Whereas ibrutinib is typically recognized as the first-in-class BTK inhibitor, acalabrutinib is considered a second generation BTK inhibitor primarily because it demonstrates highter selectivity and inhibition of the targeted activity of BTK while having a much greater IC50 or otherwise virtually no inhibition on the kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1. In effect, acalabrutinib was rationally designed to be more potent and selective than ibrutinib, all the while demonstrating fewer adverse effects - in theory - because of the drug's minimized off target effects.


API Reference Price

read-more
read-more
[{"dataSource":"API Export","activeIngredients":"ACALABRUTINIB","year":"2021","qtr":"Q1","strtotime":1616178600,"product":"ACALABRUTINIB-(SL NO:1597 OF APPENDIX 3B -MEIS)","address":"8-3-167\/D\/16, KALYAN NAGAR - I,VENGAL RAO NAGAR","city":"HYDERABAD, A.P.","supplier":"MSN LABORATORIES","supplierCountry":"INDIA","foreign_port":"DUBAI","customer":"GULF AGENCY COMPANY ","customerCountry":"UNITED ARAB EMIRATES","quantity":"1.20","actualQuantity":"1.2","unit":"KGS","unitRateFc":"21332.5","totalValueFC":"25334.8","currency":"USD","unitRateINR":1537006.2,"date":"20-Mar-2021","totalValueINR":"1844407.44","totalValueInUsd":"25334.8","indian_port":"HYDERABAD AIR","hs_no":"29400000","bill_no":"9517261","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"UNITED ARAB EMIRATES","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"8-3-167\/D\/16, KALYAN NAGAR - I,VENGAL RAO NAGAR, HYDERABAD, A.P.","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2021","qtr":"Q4","strtotime":1638469800,"product":"ACALABRUTINIB (API) (6 TLP)","address":"INSPIRE BKC PART OF 601 AND 701,BA NDRAKURLA COMPLEX BANDRA EAST","city":"MUMBAI,MAHARASHTRA","supplier":"NOVARTIS PHARMACEUTICALS CORPORATION","supplierCountry":"INDIA","foreign_port":"NEW YORK","customer":"SHARON LIN, ESQ.","customerCountry":"UNITED STATES","quantity":"0.15","actualQuantity":"150","unit":"GMS","unitRateFc":"2434.2","totalValueFC":"4786.1","currency":"INR","unitRateINR":2406.6666666666665,"date":"03-Dec-2021","totalValueINR":"361000","totalValueInUsd":"4786.1","indian_port":"HYDERABAD AIR","hs_no":"29333990","bill_no":"6470981","productDescription":"API","marketType":"REGULATED MARKET","country":"UNITED STATES","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"INSPIRE BKC PART OF 601 AND 701,BA NDRAKURLA COMPLEX BANDRA EAST, MUMBAI,MAHARASHTRA","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2022","qtr":"Q3","strtotime":1659897000,"product":"ACALABRUTINIB (QTY:2.5 KGS)","address":"MSN HOUSE, PLOT NO. C-24,INDUSTRIAL HYDERABAD","city":"HYDERABAD","supplier":"MSN LABORATORIES","supplierCountry":"INDIA","foreign_port":"HONG KONG","customer":"TO THE ORDER OF","customerCountry":"CHINA","quantity":"2.50","actualQuantity":"2.5","unit":"KGS","unitRateFc":"35000","totalValueFC":"85035.1","currency":"USD","unitRateINR":2706400,"date":"08-Aug-2022","totalValueINR":"6766000","totalValueInUsd":"85035.1","indian_port":"HYDERABAD AIR","hs_no":"29400000","bill_no":"3370692","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"MSN HOUSE, PLOT NO. C-24,INDUSTRIAL HYDERABAD, HYDERABAD","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2023","qtr":"Q2","strtotime":1688063400,"product":"MSN PHARMA -ACALABRUTINIB","address":"MSN HOUSE, PLOT NO. C-24,INDUSTRIAL HYDERABAD","city":"HYDERABAD","supplier":"MSN LABORATORIES","supplierCountry":"INDIA","foreign_port":"HONG KONG","customer":"TO THE ORDER OF","customerCountry":"CHINA","quantity":"1.50","actualQuantity":"1.5","unit":"KGS","unitRateFc":"35000","totalValueFC":"51717.7","currency":"USD","unitRateINR":2833999.8959999997,"date":"30-Jun-2023","totalValueINR":"4250999.844","totalValueInUsd":"51717.7","indian_port":"HYDERABAD AIR","hs_no":"29400000","bill_no":"0","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"MSN HOUSE, PLOT NO. C-24,INDUSTRIAL HYDERABAD, HYDERABAD","customerAddress":""}]
20-Mar-2021
30-Jun-2023
KGS
overview
Loading...

Average Price (USD/KGS)

Number of Transactions

Total Quantity (KGS)

Total Value (USD)

Quantity (KGS) & Unit rate (USD/KGS) over time

API Imports and Exports

Importing Country Total Quantity
(KGS)
Average Price
(USD/KGS)
Number of Transactions

Upgrade, download data, analyse, strategize, subscribe with us contact

FDA Orange Book

read-more
read-more

01

SupplySide West 2024
Not Confirmed
arrow
arrow
SupplySide West 2024
Not Confirmed

ACALABRUTINIB

Brand Name : ACALABRUTINIB

Dosage Form : CAPSULE;ORAL

Dosage Strength : 100MG

Approval Date :

Application Number : 216775

RX/OTC/DISCN :

RLD :

TE Code :

blank

02

ASTRAZENECA

United Kingdom
SupplySide West 2024
Not Confirmed
arrow

ASTRAZENECA

United Kingdom
arrow
SupplySide West 2024
Not Confirmed

ACALABRUTINIB

Brand Name : CALQUENCE

Dosage Form : CAPSULE;ORAL

Dosage Strength : 100MG

Approval Date : 2017-10-31

Application Number : 210259

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

blank

03

ASTRAZENECA

United Kingdom
SupplySide West 2024
Not Confirmed
arrow

ASTRAZENECA

United Kingdom
arrow
SupplySide West 2024
Not Confirmed

ACALABRUTINIB MALEATE

Brand Name : CALQUENCE

Dosage Form : TABLET;ORAL

Dosage Strength : EQ 100MG BASE

Approval Date : 2022-08-03

Application Number : 216387

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

blank
Full Screen ViewFULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]

Related Excipient Companies

Upload your portfolio for free, ask us

Excipients by Applications

Click here to find the perfect excipient manufacturers by their capabilities

Fillers, Diluents & Binders

read-more
read-more

Direct Compression

read-more
read-more

Disintegrants & Superdisintegrants

read-more
read-more

Thickeners and Stabilizers

read-more
read-more

Lubricants & Glidants

read-more
read-more

Co-Processed Excipients

read-more
read-more

Empty Capsules

read-more
read-more

Coating Systems & Additives

read-more
read-more

Granulation

read-more
read-more

Taste Masking

read-more
read-more

Controlled & Modified Release

read-more
read-more

Chewable & Orodispersible Aids

read-more
read-more

Emulsifying Agents

read-more
read-more

Film Formers & Plasticizers

read-more
read-more

Coloring Agents

read-more
read-more

Rheology Modifiers

read-more
read-more

API Stability Enhancers

read-more
read-more

Digital Content read-more

Create Content with PharmaCompass, ask us

DATA COMPILATION #PharmaFlow

read-more
read-more

NEWS #PharmaBuzz

read-more
read-more

Global Sales Information

Do you need Business Intel? Ask us

Patents & EXCLUSIVITIES

Check the patents & exclusivity for this product

ABOUT THIS PAGE

Ask Us for Pharmaceutical Supplier and Partner
Ask Us, Find A Supplier / Partner
No Commissions, No Strings Attached, Get Connected for FREE

What are you looking for?

How can we help you?

The request can't be empty

Please read our Privacy Policy carefully

You must agree to the privacy policy

The name can't be empty
The company can't be empty.
The email can't be empty Please enter a valid email.
The mobile can't be empty