Isavuconazonium
Clinical data | |
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Trade names | Cresemba |
AHFS/Drugs.com | Monograph |
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Pregnancy category |
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intravenous (IV) | |
ATC code |
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Identifiers | |
JSmol) | |
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(what is this?) (verify) |
Clinical data | |
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Trade names | Cresemba |
Other names | BAL8557 |
Pregnancy category |
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intravenous (IV) | |
ATC code | |
Legal status | |
Legal status |
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Identifiers | |
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JSmol) | |
Melting point | 122[11] °C (252 °F) |
Solubility in water | 14.2 ± 0.5 × 10−6 mol/L (pH 7.4)[11] |
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Isavuconazonium sulfate, sold under the brand name Cresemba, is a
The most common side effects include abnormal liver tests, nausea, vomiting, difficulty breathing, abdominal pain, diarrhea, injection site reactions, headache, low blood potassium and skin rash.[10]
Isavuconazonium is a
Medical uses
Isavuconazonium is used to treat invasive aspergillosis and invasive mucormycosis in adults aged eighteen years old and older. It is available in a capsule for administration by mouth and as a powder for administration via infusion.[9][7][8][12][14]
Contraindications
Isavuconazonium is contraindicated in people taking strong CYP3A4 inhibitors, strong CYP3A4 inducers, or moderate CYP3A4 or CYP3A5 inducers.[7][8][9] It is contraindicated in people with familial short QT syndrome.[7][8][9]
Side effects
Common adverse effects (occurring in between 1 and 10% of people) include
In preclinical studies, isavuconazonium caused birth defects in animals; it has not been tested in pregnant women.[7][8][9]
Interactions
Isavuconazonium is converted into isavuconazole inside the body, and isavuconazole is a substrate for CYP3A4 or CYP3A5. Many other medications inhibit or induce those two enzymes, and isavuconazonium should not be administered with them. Inducers result in levels of isavuconazole that are too low and won't work, and inhibitors can cause high levels of isavuconazole which will in turn cause increased adverse events and toxicity. Likewise isavuconazonium can interfere with appropriate dosing of other drugs that are substrates for those enzymes.[7][8]
In addition, isavuconazole induces
Pharmacology
After oral or intravenous (IV) administration, isavuconazonium is rapidly hydrolysed by esterases in blood or the gastrointestinal tract to the active form, isavuconazole.[7][8][15]
Isavuconazole works by
Chemistry
Isavuconazonium comprises an N-(3-acetoxypropyl)-N-methylamino-carboxymethyl group linked through an ester moiety to the triazole nitrogen in isavuconazole.[16][17][18] In the aquatic media of the body, the isavuconazole molecule is transformed into monohydrate.[11]
History
Isavuconazole and isavuconazonium were discovered in Japan by researchers at
In 2014, Basilea and Astellas amended the agreement to give Astellas sole marketing authority in North America, and Basilea the rights to market in the rest of the world.[23]
The U.S. Food and Drug Administration (FDA) granted approval in March 2015,[15][24] and the European Medicines Agency (EMA) approved it in October 2015.[10][7][8]
In 2017, Basilea licensed rights to Pfizer to market isavuconazole in Europe and other regions.[25][26][27]
References
- ^ a b "Isavuconazonium (Cresemba) Use During Pregnancy". Drugs.com. 31 January 2020. Retrieved 26 August 2020.
- ^ "Cresemba isavuconazole (as isavuconazonium sulfate) 200 mg powder for injection vial". Therapeutic Goods Administration (TGA). ARTG ID 305480. Archived from the original on 19 June 2022. Retrieved 5 September 2021.
- ^ "Cresemba isavuconazole (as isavuconazonium sulfate) 100 mg capsule blister pack". Therapeutic Goods Administration (TGA). ARTG ID 305452. Archived from the original on 5 September 2021. Retrieved 5 September 2021.
- ^ "AusPAR: Isavuconazole (as sulphate)". Therapeutic Goods Administration (TGA). 22 January 2020. Retrieved 5 September 2021.
- ^ "Regulatory Decision Summary for Cresemba". Drug and Health Product Register. 23 October 2014.
- ^ "Drug and medical device highlights 2018: Helping you maintain and improve your health". Health Canada. 14 October 2020. Retrieved 17 April 2024.
- ^ a b c d e f g h i j k l "Cresemba 100 mg hard capsules - Summary of Product Characteristics (SmPC)". (emc). 28 June 2021. Retrieved 5 September 2021.
- ^ a b c d e f g h i j k l "Cresemba 200mg Powder for concentrate for solution for infusion - Summary of Product Characteristics (SmPC)". (emc). 28 June 2021. Retrieved 5 September 2021.
- ^ a b c d e f "Cresemba- isavuconazonium sulfate capsule Cresemba- isavuconazonium sulfate injection, powder, lyophilized, for solution". DailyMed. 2 December 2019. Retrieved 26 August 2020.
- ^ a b c "Cresemba EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 26 August 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
- ^ S2CID 244426797.
- ^ PMID 27330318.
- ISBN 978-1-284-17132-7.
- PMID 26179012.
- ^ S2CID 208875031.
- ^ PMID 19072177.
- ^ "Proposed INN: List 96" (PDF). WHO Drug Information. 20 (4). 2006.
- ^ "Recommended INN: List 58" (PDF). WHO Drug Information. 21 (3). 2007.
- PMID 12482421.
- ^ "Isavuconazonium sulfate Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 6 May 2013. Retrieved 26 August 2020.
- ^ "Isavuconazonium sulfate Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 20 October 2014. Retrieved 26 August 2020.
- ^ "Isavuconazonium sulfate Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 25 October 2013. Retrieved 26 August 2020.
- ^ "Astellas Takes Over Isavuconazole Manufacturing and Promotion in U.S., Canada". Genetic Engineering & Biotechnology News. 28 February 2014.
- ^ "Cresemba Capsules & Cresemba Powder for Injection". U.S. Food and Drug Administration (FDA). 6 March 2015. Retrieved 26 August 2020.
- Lay summary in: "207500Orig1s000 / 207501Orig1s000 Labeling" (PDF). Center for Drug Evaluation and Research. 2015.
- ^ Elvidge S (16 June 2017). "Pfizer builds out anti-infective reach with Basilea deal". BioPharma Dive.
- ^ "Pfizer Receives Exclusive Commercialization Rights in Europe for Cresemba, a Novel Treatment for Potentially Life-Threatening Fungal Infections Among Immunocompromised Patients". Pfizer (Press release). 14 June 2017. Retrieved 5 September 2021.
- ^ "Pfizer Enters into Agreement to Develop and Commercialize Cresemba (isavuconazole) in China and Asia Pacific Region". Pfizer (Press release). 30 November 2017. Retrieved 5 September 2021.