Atebrioz (zilurgisertib) is filed as ALK2 inhibitor. The sections below restate public label fields stored for this profile.
1. INDICATIONS AND USAGE ATEBRIOZ is indicated to reduce the volume of total new heterotopic ossification (HO) in adults and pediatric patients aged 12 years and older with fibrodysplasia ossificans progressiva (FOP). ATEBRIOZ is an activin receptor-like kinase-2 (ALK2) inhibitor indicated to reduce the volume of total new heterotopic ossification (HO) in adults and pediatric patients aged 12 years and older with fibrodysplasia ossificans progressiva (FOP). (1)
12.1. Mechanism of Action FOP is a progressive disease caused by a monoallelic gain-of-function mutation in the activin A receptor, Type I (ACVR1) gene that codes the ALK2 Type I receptor in the bone morphogenetic protein (BMP) signaling pathway. Patients with FOP have constitutively active ALK2 signaling that causes HO. Zilurgisertib is an oral, and selective inhibitor of both wild-type ALK2 and pathogenic ALK2 (R206H mutation). Target engagement of zilurgisertib inhibits ALK2 mediated signaling and reduces endochondral bone formation.
5. WARNINGS AND PRECAUTIONS Embryo-Fetal Toxicity: Can cause fetal harm. Verify females of reproductive potential are not pregnant prior to initiating ATEBRIOZ and advise of the potential risk to a fetus and to use effective contraception. Advise the patient to discontinue ATEBRIOZ immediately if pregnancy occurs during treatment and to contact their healthcare provider. (5.1, 8.1, 8.3) 5.1. Embryo-Fetal Toxicity ATEBRIOZ is contraindicated during pregnancy. Based on its mechanism of action and findings from animal reproduction studies, ATEBRIOZ can cause fetal harm when administered to a pregnant woman. Oral administration of zilurgisertib to pregnant rats during the period of organogenesis resulted in adverse outcomes, including embryofetal lethality, decreased fetal weight, and skeletal malformations at exposures ≥ 3-times the human exposure at the clinical dose of 100 mg. [see Use in Specific Populations (8.1) and Clinical Pharmacology (12.1)]. For females of reproductive potential, verify that the patient is not pregnant prior to initiation of treatment. Advise females of reproductive potential to use effective contraception during treatment with ATEBRIOZ and for one week after the final dose. Advise patients to discontinue ATEBRIOZ immediately if pregnancy occurs during treatment and to contact their healthcare provider [see Use in Specific Populations (8.1, 8.3)].
4. CONTRAINDICATIONS ATEBRIOZ is contraindicated in pregnancy. ATEBRIOZ can cause fetal harm when administered to a pregnant woman [see Warnings and Precautions (5.1) and Use in Specific Populations (8.1, 8.3)]. Pregnancy. (4, 5.1, 8.1)
Headache (≥10%); Arthralgia (≥10%); Upper respiratory tract infection (≥10%); Epistaxis (≥10%); Nausea (≥10%)
6. ADVERSE REACTIONS Most common adverse reactions (≥ 10%): headache, arthralgia, upper respiratory tract infection, epistaxis, and nausea. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Mirum Pharmaceuticals, Inc. at 1-855-MRM-4YOU or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1. Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of ATEBRIOZ was evaluated in a 24-week, multicenter, randomized, double-blind, placebo-controlled trial (Study 1; NCT05090891). Sixty-three patients (28 adults and 35 pediatric patients 12 years of age and older) with FOP were randomized to ATEBRIOZ 100 mg (n = 32) or placebo (n = 31) once daily for 24 weeks. Patients who completed the 24‑week double‑blind period entered the 292-week open-label extension [see Clinical Studies (14)]. The adverse reactions reported by ≥ 10% of ATEBRIOZ-treated adults and pediatric patients aged 12 years and older and more frequently than placebo through Week 24 are listed in Table 1. Table 1: Adverse Reactions Occurring in ≥ 10% of Adults and Pediatric Patients Aged 12 Years and Older with FOP Receiving ATEBRIOZ and more Frequently than Placebo in Study 1 Through Week 24 Adverse Reaction ATEBRIOZ (N = 32) n (%) Placebo (N = 31) n (%) Headache 7 (22) 5 (16) Arthralgia 7 (22) 3 (10) Upper respiratory tract infection 7 (22) 3 (10) Epistaxis 4 (13) 0 Nausea 4 (13) 1 (3) Clinically Significant Adverse Reactions Occurring in < 10% of Patients with FOP In patients receiving ATEBRIOZ 100 mg orally once daily through Week 24, adverse reactions occurring in < 10% of patients included gastroenteritis, gastroesophageal reflux disease, iron deficiency anemia, rash (3 patients each), and alopecia (2 patients). None of these events were reported in the placebo group. Laboratory Findings Increases in Serum Iron, Hemoglobin, and Transferrin Saturation Compared to placebo, ATEBRIOZ-treated patients experienced mean increases in serum iron, hemoglobin, and transferrin saturation levels; the mean values for all three measures remained within the normal range. No significant differences in mean ferritin change from baseline was observed between ATEBRIOZ- and placebo-treated patients, including patients who took iron supplements. Based on the data through Week 100, the increases in serum iron and transferrin saturation with ATEBRIOZ were not associated with signs or symptoms of iron overload.
2. DOSAGE AND ADMINISTRATION •Recommended starting dosage: 100 mg orally once daily with or without food. (2.2) •Administer ATEBRIOZ tablets whole or crushed. If crushed, mix 4 tablets (100 mg total) with four tablespoons (60 mL) of water, orange juice, apple sauce, or plain yogurt. (2.2) 2.1. Pregnancy Testing Prior to Treatment with ATEBRIOZ Verify that females of reproductive potential are not pregnant prior to initiating ATEBRIOZ [see Contraindications (4), Warnings and Precautions (5.1), and Use in Specific Populations (8.1, 8.3)]. 2.2. Recommended Dosage and Administration The recommended dosage of ATEBRIOZ is 100 mg orally once daily with or without food [see Clinical Pharmacology (12.3)]. Administer ATEBRIOZ tablets whole or crushed. If crushed, mix 4 tablets (100 mg total) with four tablespoons (60 mL) of water, orange juice, apple sauce, or plain yogurt and administer immediately. Do not store the mixture for future use. Do not administer ATEBRIOZ with grapefruit, pomelo, or juices containing these fruits. 2.3. Dosage Modification for CYP3A4 Inhibitors Reduce the ATEBRIOZ dosage to 50 mg orally once daily when used concomitantly with a strong CYP3A4 inhibitor. No change in ATEBRIOZ dosage is needed when used concomitantly with a mild or moderate CYP3A4 inhibitor [see Drug Interactions (7.1)].
7. DRUG INTERACTIONS CYP3A4 Inhibitors: Reduce ATEBRIOZ dosage to 50 mg orally once daily when used concomitantly with a strong CYP3A4 inhibitor. (2.3, 7.1) CYP3A4 Inducers: Avoid concomitant use of ATEBRIOZ with strong or moderate CYP3A4 inducers. (7.1) MATE1 and MATE2-K Substrates: Avoid concomitant use of ATEBRIOZ with MATE1 and MATE2-K substrates (e.g., metformin). (7.2) 7.1. Effect of Other Drugs on ATEBRIOZ Strong CYP3A4 Inhibitors Reduce the ATEBRIOZ dosage to 50 mg once daily when used concomitantly with a strong CYP3A4 inhibitor [see Dosage and Administration (2.3)]. ATEBRIOZ is a CYP3A4 substrate. Strong CYP3A4 inhibitors increase zilurgisertib exposure [see Clinical Pharmacology (12.3)], which may increase the risk of ATEBRIOZ adverse reactions. Strong and Moderate CYP3A4 Inducers Avoid concomitant use of ATEBRIOZ with strong or moderate CYP3A4 inducers. Strong or moderate CYP3A4 inducers decrease zilurgisertib plasma concentrations [see Clinical Pharmacology (12.3)], which may reduce the effectiveness of ATEBRIOZ. 7.2. Effect of ATEBRIOZ on Other Drugs MATE1 and MATE2-K Substrates Avoid concomitant use of ATEBRIOZ with MATE1 and MATE2-K substrates (e.g., metformin). If unavoidable, monitor for adverse reactions and consider dose reduction of the substrates if appropriate, according to their approved prescribing information. ATEBRIOZ is a MATE1 and MATE2-K inhibitor. ATEBRIOZ may increase exposure of substrates of MATE1 and MATE2-K, which may increase the risk of adverse events of MATE1 and MATE2-K substrates.
17. PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Medication Guide). Administration Information •Instruct patients to take ATEBRIOZ orally once daily with or without food. •Inform patients and/or caregivers that ATEBRIOZ may be swallowed whole or crushed and mixed with liquid or soft food [see Dosage and Administration (2.2)]. Embryo-Fetal Toxicity ATEBRIOZ can cause fetal harm and is contraindicated during pregnancy. Advise females to immediately stop ATEBRIOZ and contact their healthcare provider if pregnancy occurs during treatment [see Warnings and Precautions (5.1) and Use in Specific Populations (8.1)]. Advise female patients of reproductive potential to use effective contraception, during treatment with ATEBRIOZ and for one week after the final dose [see Use in Specific Populations (8.3)]. Lactation Advise females not to breastfeed during treatment with ATEBRIOZ and for at least one week after the final dose [see Use in Specific Populations (8.2)]. Drug Interactions Advise patients to inform their healthcare providers of all concomitant medications, herbal and dietary supplements [see Drug Interactions (7.1)]. Manufactured for:Mirum Pharmaceuticals, Inc.Foster City, CA 94404 Licensed from:Incyte CorporationWilmington, DE 19803 ATEBRIOZ is a trademark of Incyte. © 2026 Mirum Pharmaceuticals, Inc. All rights reserved. LB00332v1
According to its FDA label, Atebrioz (zilurgisertib) is approved for: 1. INDICATIONS AND USAGE ATEBRIOZ is indicated to reduce the volume of total new heterotopic ossification (HO) in adults and pediatric patients aged 12 years and older with fibrodysplasia ossificans progressiva (FOP). ATEBRIOZ is an activin receptor-like kinase-2 (ALK2) inhibitor… For medical advice, please talk to your prescriber or pharmacist.
Atebrioz (zilurgisertib) belongs to the ALK2 inhibitor class of medications.
The FDA label lists Atebrioz (zilurgisertib) as: 3. DOSAGE FORMS AND STRENGTHS ATEBRIOZ Tablets: 25 mg of zilurgisertib, film-coated, white to off-white, round, debossed with "INCY" on one side and "25" on the other side. Tablets: 25 mg of zilurgisertib. (3); oral route. Available strengths and packaging vary by manufacturer.
Not yet. As of the most recent FDA data we ingest, no A-rated generic equivalent is listed for Atebrioz. Availability changes as patents expire.
Our ingest of the FDA label for Atebrioz (zilurgisertib) does not include a Boxed Warning at this time. See the full label on DailyMed for the current, authoritative version.
The FDA Enforcement Report does not show an active/ongoing recall for Atebrioz (zilurgisertib) in our latest ingest. Recall data can change daily — verify at FDA.gov.
The FDA record lists the approval date for Atebrioz (zilurgisertib) as 2026-09-25.
The FDA label lists Mirum Pharmaceuticals Inc. as a labeler/manufacturer of Atebrioz (zilurgisertib). Multiple firms may market generics of the same molecule.
The FDA label states: "16. HOW SUPPLIED/STORAGE AND HANDLING How Supplied ATEBRIOZ contains 25 mg of zilurgisertib and is available as a round, white to off-white film‑coated tablet debossed on one side with "INCY" and "25" on the other side i…" Follow the packaging insert for the authoritative guidance.
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