Infigratinib

Last updated

Infigratinib
Infigratinib.png
Clinical data
Trade names Truseltiq
Other namesBGJ-398
AHFS/Drugs.com Monograph
MedlinePlus a621041
License data
Pregnancy
category
Routes of
administration 		By mouth
Drug class Tyrosine kinase inhibitor
ATC code
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
Formula C26H31Cl2N7O3
Molar mass 560.48 g·mol−1
3D model (JSmol)
  • CCN1CCN(c2ccc(Nc3cc(N(C)C(=O)Nc4c(Cl)c(OC)cc(OC)c4Cl)ncn3)cc2)CC1
  • InChI=1S/C26H31Cl2N7O3/c1-5-34-10-12-35(13-11-34)18-8-6-17(7-9-18)31-21-15-22(30-16-29-21)33(2)26(36)32-25-23(27)19(37-3)14-20(38-4)24(25)28/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31)
  • Key:QADPYRIHXKWUSV-UHFFFAOYSA-N

Infigratinib, sold under the brand name Truseltiq, is an anti-cancer medication used to treat cholangiocarcinoma (bile duct cancer). [1] [4]

Contents

The most common side effects include increased phosphate level in the blood, increased creatinine levels in the blood, nail changes, mouth sores, dry eye, fatigue, alopecia, and palmar-plantar erythrodysesthesia (rash, redness, pain, swelling or blisters on the palms of the hands or soles of the feet). [5] [6]

Infigratinib is a kinase inhibitor targeting the fibroblast growth factor receptors FGFR1, FGFR2, and FGFR3. [4] [7]

Infigratinib was approved for medical use in the United States in May 2021. [4] [5] [6] [8] [9]

Medical uses

Infigratinib is indicated for the treatment of adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma (bile duct cancer) with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement as detected by an FDA-approved test. [4] [5]

Adverse effects

The most common side effects include increased phosphate level in the blood, increased creatinine levels in the blood, nail changes, mouth sores, dry eye, fatigue, alopecia, and palmar-plantar erythrodysesthesia (rash, redness, pain, swelling or blisters on the palms of the hands or soles of the feet ). [5]

Infigratinib may cause serious side effects including detachment of retina (inner layer of the eye), increased phosphate level in the blood, and harm to an unborn baby. [5]

History

The US Food and Drug Administration (FDA) approved infigratinib based on evidence from one clinical trial (NCT02150967) of 108 participants with bile duct cancer (cholangiocarcinoma). [5] The CBGJ398X2204 trial was a multicenter open-label single-arm trial that enrolled 108 participants with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with an FGFR2 fusion or rearrangement as determined by local or central testing. [6] The trials were conducted at 18 sites in the United States, Europe, and Asia. [5] The trial enrolled adult participants with bile duct cancer who had been treated previously with chemotherapy for their advanced cancer and whose tumors had a certain type of abnormality in the FGFR2 gene. [5] Participants received infigratinib once daily by mouth for 21 consecutive days followed by 7 days off therapy. [5] This 28-day cycle was administered until disease progression or the side effects became too toxic. [5] The trial measured the percentage of participants who achieved partial or complete shrinkage of their cancer and how long that shrinkage lasted (duration of response or DoR). [5]

The FDA granted the application for infigratinib priority review, fast track, and orphan drug designations. [6]

Society and culture

Infigratinib was designated an orphan drug by the FDA [10] and the European Medicines Agency in 2021. [11] It was approved for medical use under the FDA's accelerated approval program in May 2021. [5] [6]

Related Research Articles

<span class="mw-page-title-main">Cholangiocarcinoma</span> Bile duct adenocarcinoma

Cholangiocarcinoma, also known as bile duct cancer, is a type of cancer that forms in the bile ducts. Symptoms of cholangiocarcinoma may include abdominal pain, yellowish skin, weight loss, generalized itching, and fever. Light colored stool or dark urine may also occur. Other biliary tract cancers include gallbladder cancer and cancer of the ampulla of Vater.

<span class="mw-page-title-main">Lenvatinib</span> Chemical compound

Lenvatinib, sold under the brand name Lenvima among others, is an anti-cancer medication for the treatment of certain kinds of thyroid cancer and for other cancers as well. It was developed by Eisai Co. and acts as a multiple kinase inhibitor against the VEGFR1, VEGFR2 and VEGFR3 kinases.

<span class="mw-page-title-main">Nivolumab</span> Cancer drug

Nivolumab, sold under the brand name Opdivo, is a medication used to treat a number of types of cancer. This includes melanoma, lung cancer, malignant pleural mesothelioma, renal cell carcinoma, Hodgkin lymphoma, head and neck cancer, urothelial carcinoma, colon cancer, esophageal squamous cell carcinoma, liver cancer, gastric cancer, and esophageal or gastroesophageal junction (GEJ) cancer. It is used by slow injection into a vein.

Margetuximab, sold under the brand name Margenza, is a chimeric IgG monoclonal antibody medication against HER2 used for the treatment of cancer.

<span class="mw-page-title-main">Pembrolizumab</span> Pharmaceutical drug used in cancer treatment

Pembrolizumab, sold under the brand name Keytruda, is a humanized antibody used in cancer immunotherapy that treats melanoma, lung cancer, head and neck cancer, Hodgkin lymphoma, stomach cancer, cervical cancer, and certain types of breast cancer. It is given by slow injection into a vein.

Enfortumab vedotin, sold under the brand name Padcev, is an antibody-drug conjugate used for the treatment of urothelial cancer. It is a nectin-4-directed antibody and microtubule inhibitor conjugate. Enfortumab refers to the monoclonal antibody part, and vedotin refers to the payload drug (MMAE) and the linker.

<span class="mw-page-title-main">Atezolizumab</span> Monoclonal anti-PD-L1 antibody

Atezolizumab, sold under the brand name Tecentriq, is a monoclonal antibody medication used to treat urothelial carcinoma, non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), hepatocellular carcinoma and alveolar soft part sarcoma, but discontinued for use in triple-negative breast cancer (TNBC). It is a fully humanized, engineered monoclonal antibody of IgG1 isotype against the protein programmed cell death-ligand 1 (PD-L1).

<span class="mw-page-title-main">Sacituzumab govitecan</span> Antibody-drug conjugate

Sacituzumab govitecan, sold under the brand name Trodelvy, is a Trop-2-directed antibody and topoisomerase inhibitor drug conjugate used for the treatment of metastatic triple-negative breast cancer and metastatic urothelial cancer.

<span class="mw-page-title-main">Tucatinib</span> Chemical compound

Tucatinib, sold under the brand name Tukysa, is an anticancer medication used for the treatment of HER2-positive breast cancer. It is a small molecule inhibitor of HER2. It was developed by Array BioPharma and licensed to Cascadian Therapeutics.

<span class="mw-page-title-main">Erdafitinib</span> Chemical compound

Erdafitinib, sold under the brand name Balversa, is an anti-cancer medication. It is a small molecule inhibitor of fibroblast growth factor receptor (FGFR) used for the treatment of cancer. FGFRs are a subset of tyrosine kinases which are unregulated in some tumors and influence tumor cell differentiation, proliferation, angiogenesis, and cell survival. Astex Pharmaceuticals discovered the drug and licensed it to Janssen Pharmaceuticals for further development.

<span class="mw-page-title-main">Ivosidenib</span> Anti-cancer medication

Ivosidenib, sold under the brand name Tibsovo, is an anti-cancer medication for the treatment of acute myeloid leukemia (AML) and cholangiocarcinoma. It is a small molecule inhibitor of isocitrate dehydrogenase-1 (IDH1), which is mutated in several forms of cancer. Ivosidenib is an isocitrate dehydrogenase-1 inhibitor that works by decreasing abnormal production of the oncometabolite 2-hydroxyglutarate (2-HG), leading to differentiation of malignant cells.

<span class="mw-page-title-main">Tepotinib</span> Chemical compound

Tepotinib, sold under the brand name Tepmetko, is an anti-cancer medication used for the treatment of adults with non-small cell lung cancer (NSCLC).

<span class="mw-page-title-main">Trastuzumab deruxtecan</span> Medication

Trastuzumab deruxtecan, sold under the brand name Enhertu, is an antibody-drug conjugate consisting of the humanized monoclonal antibody trastuzumab (Herceptin) covalently linked to the topoisomerase I inhibitor deruxtecan. It is licensed for the treatment of breast cancer or gastric or gastroesophageal adenocarcinoma. Trastuzumab binds to and blocks signaling through epidermal growth factor receptor 2 (HER2/neu) on cancers that rely on it for growth. Additionally, once bound to HER2 receptors, the antibody is internalized by the cell, carrying the bound deruxtecan along with it, where it interferes with the cell's ability to make DNA structural changes and replicate its DNA during cell division, leading to DNA damage when the cell attempts to replicate itself, destroying the cell.

<span class="mw-page-title-main">Pemigatinib</span> Pharmaceutical drug

Pemigatinib, sold under the brand name Pemazyre, is an anti-cancer medication used for the treatment of bile duct cancer (cholangiocarcinoma). Pemigatinib works by blocking FGFR2 in tumor cells to prevent them from growing and spreading.

<span class="mw-page-title-main">Selpercatinib</span> Chemical compound

Selpercatinib, sold under the brand name Retevmo among others, is a medication for the treatment of cancers in people whose tumors have an alteration in a specific gene. It is taken by mouth.

<span class="mw-page-title-main">Ripretinib</span> Chemical compound

Ripretinib, sold under the brand name Qinlock, is a medication for the treatment of adults with advanced gastrointestinal stromal tumor (GIST), a type of tumor that originates in the gastrointestinal tract. It is taken by mouth. Ripretinib inhibits the activity of the kinases KIT and PDGFRA, which helps keep cancer cells from growing.

Pralsetinib, sold under the brand name Gavreto, is a medication approved for RET mutation-positive medullary thyroid cancer (MTC) and RET fusion-positive differentiated thyroid cancer (DTC) refractory to radioactive iodine (RAI) therapy. Pralsetinib is a tyrosine kinase inhibitor. It is taken by mouth.

Tebentafusp, sold under the brand name Kimmtrak, is an anti-cancer medication used to treat uveal melanoma. Tebentafusp is a bispecific gp100 peptide-HLA-directed CD3 T cell engager. Tebentafusp is given by intravenous infusion.

<span class="mw-page-title-main">Futibatinib</span> Chemical compound

Futibatinib, sold under the brand name Lytgobi, is an anti-cancer medication used for the treatment of cholangiocarcinoma. It is a kinase inhibitor. It is taken by mouth.

<span class="mw-page-title-main">Fruquintinib</span> Medication

Fruquintinib, sold under the brand name Fruzaqla, is an anti-cancer medication used for the treatment of colorectal cancer. Fruquintinib is a kinase inhibitor.

References

  1. 1 2 3 "Truseltiq". Therapeutic Goods Administration (TGA). 22 November 2021. Retrieved 28 December 2021.
  2. ↑ "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 12 May 2022. Archived from the original on 3 April 2022. Retrieved 13 May 2022.
  3. ↑ "Summary Basis of Decision (SBD) for Truseltiq". Health Canada. 23 October 2014. Archived from the original on 29 May 2022. Retrieved 29 May 2022.
  4. 1 2 3 4 5 "Truseltiq- infigratinib capsule". DailyMed. Archived from the original on 10 June 2021. Retrieved 10 June 2021.
  5. 1 2 3 4 5 6 7 8 9 10 11 12 "Drug Trials Snapshots: Truseltiq". U.S. Food and Drug Administration (FDA). 28 May 2021. Archived from the original on 28 July 2023. Retrieved 1 August 2023.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  6. 1 2 3 4 5 "FDA grants accelerated approval to infigratinib for metastatic cholang". U.S. Food and Drug Administration. 28 May 2021. Archived from the original on 2 August 2023. Retrieved 1 August 2023.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  7. ↑ Botrus G, Raman P, Oliver T, Bekaii-Saab T (April 2021). "Infigratinib (BGJ398): an investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma". Expert Opinion on Investigational Drugs. 30 (4): 309–316. doi:10.1080/13543784.2021.1864320. PMID   33307867. S2CID   229177726.
  8. ↑ "BridgeBio Pharma's Affiliate QED Therapeutics and Partner Helsinn Group Announce FDA Approval of Truseltiq (infigratinib) for Patients with Cholangiocarcinoma" (Press release). BridgeBio Pharma. 28 May 2021. Retrieved 28 May 2021– via GlobeNewswire.
  9. ↑ Advancing Health Through Innovation: New Drug Therapy Approvals 2021 (PDF). U.S. Food and Drug Administration (FDA) (Report). 13 May 2022. Archived from the original on 6 December 2022. Retrieved 22 January 2023.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  10. ↑ "Infigratinib Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 11 September 2019. Archived from the original on 28 October 2022. Retrieved 30 May 2021.
  11. ↑ "EU/3/21/2475". European Medicines Agency. 13 June 2022. Archived from the original on 30 May 2023. Retrieved 1 August 2023.
This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.