USA Domestic Delivery,Canada Domestic Delivery,European Domestic Delivery

Ibrutinib

Rating: Category:

Ibrutinib blocks a protein called Bruton’s tyrosine kinase (BTK), which may help keep cancer cells from growing. It is a type of tyrosine kinase inhibitor. Also called Imbruvica.

Product Description

Basic Characteristics

Product Name Ibrutinib
CAS Number 936563-96-1
Molecular Formula C25H24N6O2
Formula Weight 440.5
Synonyms IBRUTINIB (PCI-32765);

(R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo-[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-;PCI-32765 (Ibrutinib);

1[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1Hpyrazolo [3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one).

Appearance White to off-white powder
Storage and Handling Store in the original, labeled container at room temperature and in a dry location.

 

Ibrutinib Description

Ibrutinib is a type of drug which was used alone or with other drugs to treat adults with chronic lymphocytic leukemia, small lymphocytic lymphoma, or Waldenstrom macroglobulinemia (a type of non-Hodgkin lymphoma). It is also used alone to treat adults with mantle cell lymphoma or marginal zone lymphoma who have received at least one other treatment. It is also being studied in the treatment of other types of cancer. Ibrutinib blocks a protein called Bruton’s tyrosine kinase (BTK), which may help keep cancer cells from growing. It is a type of tyrosine kinase inhibitor. Also called Imbruvica.

 

Ibrutinib Mechanism of Action

Ibrutinib is a potent and irreversible inhibitor of Bruton’s tyrosine kinase (BTK), an integral component of the B-cell receptor (BCR) and cytokine receptor pathways. Constitutive activation of B-cell receptor signaling is important for survival of malignant B-cells; BTK inhibition results in decreased malignant B-cell proliferation and survival.

 

Ibrutinib Application

Ibrutinib is approved in Europe for treating three types of lymphoma.

 

♦ Mantle cell lymphoma

For people whose lymphoma has relapsed (come back) or has not responded to treatment (refractory lymphoma). Ibrutinib is given on its own.

 

♦ Chronic lymphocytic leukaemia (CLL)

For people who have not yet had treatment for their CLL (first-line treatment). Ibrutinib can be given on its own or in combination with rituximab  or obinutuzumab (antibody therapies). For people whose CLL has relapsed after treatment. For people with relapsed CLL, ibrutinib can be given on its own or with bendamustine (a chemotherapy drug) and rituximab.

 

♦ Waldenström’s macroglobulinaemia (WM)

For people who have previously received other treatments for WM. For people who can’t have chemo-immunotherapy (chemotherapy with antibody therapy) as first-line treatment.

European approval to use ibrutinib in CLL and mantle cell lymphoma was granted in November 2014. It was then extended to WM in May 2015. In 2016, the European Medicines Agency (EMA) expanded ibrutinib’s recommended uses for CLL.

Ibrutinib is being tested in further clinical trials in people with these types of lymphoma. This is to see if ibrutinib could work better in combination with other treatments, such as chemotherapy or antibody therapy (for example, rituximab). It is also being tested in other types of lymphoma. Use our searchable database to see if there’s a clinical trial that might be suitable for you at Lymphoma TrialsLink.

 

Ibrutinib Side Effects & Warning

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using ibrutinib and call your doctor at once if you have:

▪ signs of infection–fever, chills, weakness, mouth sores, cough with mucus, trouble breathing;

▪ signs of bleeding inside your body–dizziness, weakness, confusion, problems with speech, prolonged headache, black or bloody stools, pink or brown urine, or coughing up blood or vomit that looks like coffee grounds;

▪ severe or ongoing diarrhea;

▪ chest pain, pounding heartbeats or fluttering in your chest, feeling like you might pass out;

▪ severe headache, blurred vision, pounding in your neck or ears;

▪ easy bruising, unusual bleeding, purple or red spots under your skin;

▪ pale skin, cold hands and feet;

▪ kidney problems–little or no urinating, swelling in your feet or ankles; or

▪ signs of tumor cell breakdown–confusion, weakness, muscle cramps, nausea, vomiting, fast or slow heart rate, decreased urination, tingling in your hands and feet or around your mouth.

 

Common side effects may include:

▪ diarrhea, nausea;

▪ fever, cough, trouble breathing;

▪ blisters or ulcers in your mouth;

▪ feeling tired;

▪ bruising, rash; or

▪ muscle pain, bone pain.

 

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

 

Reference

[1] Ahn IE, Jerussi T, Farooqui M, Tian X, Wiestner A, Gea-Banacloche J. Atypical Pneumocystis jirovecii pneumonia in previously untreated patients with CLL on single-agent ibrutinib. Blood. 2016;128(15):1940-1943. [PubMed 27503501].

[2] Wang ML, Rule S, Martin P, et al. Targeting BTK with ibrutinib in relapsed or refractory mantle-cell lymphoma. N Engl J Med, 2013;369(6):507-516. [PubMed 23782157].

[3] Byrd JC, Furman RR, Coutre SE, et al. Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia. N Engl J Med. 2013;369(1):32-42. [PubMed 23782158].

[4] Kamel S, Horton L, Ysebaert L, et al. Ibrutinib inhibits collagen-mediated but not ADP-mediated platelet aggregation. Leukemia. 2015;29(4):783-787. [PubMed 25138588].

[5] Marostica E, Sukbuntherng J, Loury D, et al. Population pharmacokinetic model of ibrutinib, a Bruton tyrosine kinase inhibitor, in patients with B cell malignancies. Cancer Chemother Pharmacol. 2015;75(1):111-121. [PubMed 25381051].

[6] Salem JE, Manouchehri A, Bretagne M, et al. Cardiovascular toxicities associated with ibrutinib. J Am Coll Cardiol. 2019;74:1667-1678. doi: 10.1016/j.jacc.2019.07.056. [PubMed 31558250].

[7] Imbruvica (ibrutinib) [prescribing information]. Sunnyvale, CA: Pharmacyclics; April 2020..

[8] Treon SP, Tripsas CK, Meid K et al. Ibrutinib in previously treated Waldenström’s macroglobulinemia. N Engl J Med. 2015;372(15):1430-1440. [PubMed 25853747].