https://www.aasraw.com/anti-cancer-drugs-acalabrutinib/ https://www.aasraw.com/products/acalabrutinibacp-196/ Acalabrutinib powder, also known as ACP-196, is a novel irreversible second-generation Bruton’s tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway and that, was rationally designed to be more potent and selective than ibrutinib.

1. www.aasraw.com
1 AASraw Biochemical Technology Co.,Ltd
aas14@aasraw.com
What is Acalabrutinib(ACP-196)
Basic Characteristics
Product Name Acalabrutinib powder(ACP-196)
CAS Number 1420477-60-6
Molecular
Formula
C26H23N7O2
Formula Weight 465.5
Synonyms
Acalabrutinib powder;
1420477-60-6;
ACP-196;
Calquence;
UNII-I42748ELQW.
Appearance Brown powder(Tea color)
Storage and
Handling
Store in a closed container at room temperature, away
from heat, moisture, and direct light. Keep from freezing.
Acalabrutinib Powder(ACP-196)
Description
Acalabrutinib powder, also known as ACP-196, is a novel irreversible
second-generation Bruton’s tyrosine kinase (BTK) inhibitor, which
prevents the activation of the B-cell antigen receptor (BCR) signaling

2. www.aasraw.com
2 AASraw Biochemical Technology Co.,Ltd
aas14@aasraw.com
pathway and that, was rationally designed to be more potent and
selective than ibrutinib. This drug in clinical trials phase III for
treatment the treatment of relapsed chronic lymphocytic leukemia.
Also in combination with others drugs, Acalabrutinib powder in phase
II of clinical trials for the treatment Glioblastoma Multiforme, Mantle
Cell Lymphoma, Squamous Cell Carcinoma of the Head and Neck,
Rheumatoid Arthritis and some others.
Acalabrutinib Powder(ACP-196)
Mechanism of Action
Acalabrutinib powder is a small molecule inhibitor of BTK. Both
acalabrutinib powder 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 powder 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 powder 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, ERBB, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC,
and YES1.
In effect, acalabrutinib powder 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.
Acalabrutinib Powder(ACP-196)
Application
Acalabrutinib powder is used to treat people with mantle cell
lymphoma (MCL; a fast-growing cancer that begins in the cells of the

3. www.aasraw.com
3 AASraw Biochemical Technology Co.,Ltd
aas14@aasraw.com
immune system) who have already been treated with at least one
other chemotherapy medication. It is also used alone or with
obinutuzumab (Gazyva) to treat chronic lymphocytic leukemia (CLL; a
type of cancer that begins in the white blood cells) and small
lymphocytic lymphoma (SLL: a type of cancer that begins in the white
blood cells). Acalabrutinib powder is in a class of medications called
kinase inhibitors. It works by blocking the action of the abnormal
protein that signals cancer cells to multiply. This helps stop the spread
of cancer cells.
Acalabrutinib Powder(ACP-196) Side
Effects & Warning
Along with its needed effects, a medicine may cause some unwanted
effects. Although not all of these side effects may occur, if they do
occur they may need medical attention.
Check with your doctor immediately if any of the following side effects
occur:
More common
bleeding gums
collection of blood under the skin
coughing up blood
difficulty in breathing or swallowing
dizziness
headache
increased menstrual flow or vaginal bleeding

4. www.aasraw.com
4 AASraw Biochemical Technology Co.,Ltd
aas14@aasraw.com
itching, pain, redness, or swelling
large, flat, blue or purplish patches in the skin
nosebleeds
paralysis
prolonged bleeding from cuts
red or black, tarry stools
red or dark brown urine
Some side effects may occur that usually do not need medical
attention. These side effects may go away during treatment as your
body adjusts to the medicine. Also, your health care professional may
be able to tell you about ways to prevent or reduce some of these side
effects. Check with your health care professional if any of the
following side effects continue or are bothersome or if you have any
questions about them:
More common
constipation
diarrhea
difficulty in moving
joint pain or swelling
muscle cramp, pain, or stiffness
nausea

5. www.aasraw.com
5 AASraw Biochemical Technology Co.,Ltd
aas14@aasraw.com
rash
stomach pain
unusual tiredness or weakness
vomiting
Other side effects not listed may also occur in some patients. If you
notice any other effects, check with your healthcare professional. Call
your doctor for medical advice about side effects. You may report side
effects to the FDA at 1-800-FDA-1088.
Reference
[1] Fischer K Al-Sawaf O Bahlo J et al. Venetoclax and obinutuzumab
in patients with CLL and coexisting conditions.N Engl J Med. 2019;
380: 2225-2236.
[2] House DW (2016-02-25). “AstraZeneca and Acerta Pharma’s
acalabrutinib powder tagged an Orphan Drug in Europe for three
indications”. Seeking Alpha. Retrieved 2016-11-21.
[3] “EU/3/16/1626”. European Medicines Agency (EMA). 4 May 2016.
Retrieved 15 April 2020.
[4] Byrd JC, Harrington B, O’Brien S, Jones JA, Schuh A, Devereux S,
et al. (January 2016). “Acalabrutinib powder (ACP-196) in Relapsed
Chronic Lymphocytic Leukemia”. The New England Journal of
Medicine. 374 (4): 323–32.
[5] “Acalabrutinib powder Orphan Drug Designation and Approval”.
U.S. Food and Drug Administration (FDA). Retrieved 15 April 2020.
[6] Walker I, Roland D (2015-12-17). “AstraZeneca to Buy Stake in
Acerta Pharma”. Wall Street Journal. ISSN 0099-9660. Retrieved
2016-11-19.

6. www.aasraw.com
6 AASraw Biochemical Technology Co.,Ltd
aas14@aasraw.com
[7] Hallek M Fischer K Fingerle-Rowson G et al. Addition of rituximab
to fludarabine and cyclophosphamide in patients with chronic
lymphocytic leukaemia: a randomised, open-label, phase 3 trial.
Lancet. 2010; 376: 1164-1174.
[8] Burger JA Tedeschi A Barr PM et al. Ibrutinib as initial therapy for
patients with chronic lymphocytic leukemia.N Engl J Med. 2015; 373:
2425-2437.