Odomzo (sonidegib phosphate)
Antineoplastic - Hedgehog Pathway Inhibitors Oral Capsule
Last reviewed · Source: First Databank (FDB) drug data
Overview
Sonidegib, a hedgehog signaling pathway inhibitor, is an antineoplastic agent.
Sonidegib is an antineoplastic agent that inhibits the hedgehog pathway by binding to and selectively inhibiting Smoothened, a transmembrane protein involved in hedgehog signal transduction. The hedgehog signaling pathway plays an important role during embryonic organ and tissue development and is a key regulator of bone development and maintenance of tissues and stem cells in adults and during postnatal development. However, genetic mutations that allow for aberrant activation of the hedgehog pathway have been implicated in the development of several malignancies such as basal cell carcinoma.
Inhibition of Smoothened by sonidegib results in inhibition of the hedgehog pathway.
Following oral administration, less than 10% of sonidegib is absorbed. Area under the serum concentration-time curve (AUC) and peak plasma concentrations of sonidegib are dose proportional over a dosage range of 100-400 mg. Peak plasma concentrations of sonidegib are achieved 2-4 hours following oral administration of a single dose of sonidegib (100 mg to 3 g) under fasting conditions in cancer patients.
Following administration of sonidegib, steady-state concentrations of the drug are achieved in approximately 4 months and the estimated accumulation is 19-fold. Administration of sonidegib with a high-fat meal (approximately 1000 calories with 50% of calories from fat) increased systemic exposure (AUC and peak plasma concentrations) of sonidegib by 7.4- to 7.8-fold. In a population pharmacokinetic analysis, administration of sonidegib with a high-fat meal increased bioavailability of the drug fivefold.
Sonidegib is metabolized in the liver principally by cytochrome P-450 (CYP) isoenzyme 3A. In vitro, sonidegib is more than 97% bound to plasma proteins. Following oral administration of sonidegib, approximately 70% of the absorbed dose is recovered in feces and 30% is recovered in urine; unchanged drug is not excreted in urine.
The estimated plasma elimination half-life of the drug is 28-29.6 days.
Population pharmacokinetic analyses indicate that age, sex, body weight, and ethnicity generally do not have clinically important effects on the exposure of sonidegib. A cross-study comparison indicates that systemic exposure following administration of sonidegib (single 200-mg dose) is increased by 1.7-fold in healthy Japanese individuals compared with individuals from Western countries.
USES: This medication is used to treat a certain type of skin cancer (basal cell carcinoma).
Generic name: sonidegib phosphate
Pronunciation: (SOE-ni-DEG-ib)
Drug class: Antineoplastic - Hedgehog Pathway Inhibitors
Therapeutic class: Antineoplastics
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Odomzo
Indications
The following indications are listed for Odomzo:
- Basal Cell Carcinoma Of Skin
Also known as: Basal Cell Epithelioma, Basalioma.
Dosing
No dosing information is available for this tab.
Sonidegib is administered orally once daily on an empty stomach, at least 1 hour before or 2 hours after a meal.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Odomzo 200 Mg Capsule | Maintenance | Take 1 capsule (200 mg) by oral route once daily. |
No dosing information is available for this tab.
Drug interactions
Sonidegib is metabolized principally by cytochrome P-450 (CYP) isoenzyme 3A. In vitro studies indicate that sonidegib inhibits CYP isoenzymes 2B6 and 2C9, but does not induce CYP 1A2, 2B6, or 3A.
In vitro studies indicate that sonidegib inhibits breast cancer resistance protein (BCRP, ABCG2), but does not inhibit P-glycoprotein (P-gp, ABCB1), multidrug resistance protein 2 (MRP2, ABCC2), organic cation transporter (OCT) 1, OCT2, organic anion transporter (OAT) 1, OAT3, organic anion transport protein (OATP) 1B1, and OATP1B3. In vitro studies also indicate that the drug is not a substrate of P-gp, MRP2, or BCRP.
Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
Sonidegib/Strong & Moderate Cyp3a4 Inducers
SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
MECHANISM OF ACTION: Agents that induce the CYP3A4 isoenzyme may induce the metabolism of sonidegib.(1)
CLINICAL EFFECTS: Concurrent use of strong or moderate CYP3A4 inducers may decrease the levels and effectiveness of sonidegib.(1)
PREDISPOSING FACTORS: Induction effects may be more likely with regular use of the inducer for longer than 1-2 weeks.
PATIENT MANAGEMENT: Avoid the concurrent use of strong or moderate CYP3A4 inducers in patients receiving therapy with sonidegib.(1) Consider the use of alternatives with little to no induction potential.
DISCUSSION: In an interaction study, 16 healthy subjects received a single dose of sonidegib 800mg alone or 5 days after receiving rifampin 600 mg daily for 14 days. Mean sonidegib area-under-curve (AUC) was decreased by 75% and maximum concentration (Cmax) decreased 54% when taken with rifampin. Based upon population based pharmacokinetic (PBPK) simulations, a moderate CYP3A4 inducer such as efavirenz given for 14 days is predicted to decrease sonidegib AUC 56% in cancer patients taking sonidegib 200 mg daily. Coadministration with a moderate CYP3A4 inducer for 4 months is predicted to decrease sonidegib exposure (AUC) by 69%.(1) Strong inducers of CYP3A4 include: apalutamide, barbiturates, carbamazepine, encorafenib, enzalutamide, fosphenytoin, ivosidenib, lumacaftor, mitotane, phenobarbital, phenytoin, primidone, rifampin, rifapentine, and St. John's wort. Moderate inducers of CYP3A4 include: bosentan, cenobamate, dabrafenib, efavirenz, elagolix, etravirine, fexinidazole, lesinurad, lorlatinib, mavacamten, mitapivat, modafinil, nafcillin, pacritinib, pexidartinib, repotrectinib, rifabutin, sotorasib, telotristat ethyl, thioridazine, and tovorafenib.(2-3)
Sonidegib/Strong Cyp3a4 Inhibitors
SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
MECHANISM OF ACTION: Agents that inhibit the CYP3A4 isoenzyme may inhibit the metabolism of sonidegib.(1)
CLINICAL EFFECTS: Concurrent use of strong CYP3A4 inhibitors may increase levels of and effects from sonidegib, including musculoskeletal adverse reactions (elevated creatine kinase) or rhabdomyolysis.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Avoid the use of strong CYP3A4 inhibitors in patients undergoing therapy with sonidegib.(1) Consider alternatives with no or minimal enzyme inhibition.
DISCUSSION: In a study, 15 healthy subjects received a single sonidegib 800 mg alone or after ketoconazole 200 mg twice daily for 14 days. Mean area-under-curve (AUC) and concentration maximum (Cmax) increased by 2.2-fold and 1.5-fold respectively.(1) Strong inhibitors of CYP3A4 include: adagrasib, boceprevir, ceritinib, clarithromycin, cobicistat, ensitrelvir, idelalisib, indinavir, itraconazole, josamycin, ketoconazole, lonafarnib, lopinavir, mibefradil, mifepristone, nefazodone, nelfinavir, nirmatrelvir/ritonavir, paritaprevir, posaconazole, relacorilant, ribociclib, saquinavir, telaprevir, telithromycin, tipranavir, troleandomycin, tucatinib, or voriconazole.(2,3)
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Cobimetinib; Olaparib; Sonidegib/Moderate Cyp3a4 Inhibitors
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Agents which inhibit the CYP3A4 enzyme may inhibit the metabolism of cobimetinib, olaparib, and sonidegib.(1-4)
CLINICAL EFFECTS: Concurrent use of moderate CYP3A4 inhibitors may increase systemic exposure and the risk for adverse effects from cobimetinib, olaparib, or sonidegib.(1-4)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: When possible, avoid the use of moderate CYP3A4 inhibitors in patients receiving cobimetinib, olaparib, or sonidegib.(1-4) For patients taking cobimetinib 60 mg daily, if concurrent short term use (14 days or less) of a moderate CYP3A4 inhibitor cannot be avoided, reduce cobimetinib dose to 20 mg daily. After discontinuation of the moderate CYP3A4 inhibitor resume the previous 60 mg dose. Patients who are taking cobimetinib 40 mg or 20 mg daily should not receive a moderate or strong CYP3A4 inhibitor.(1) If concomitant use with olaparib cannot be avoided, reduce the olaparib dose. Dosage adjustments are specific to the formulation of olaparib.(2,3) Reduce the dosage of the CAPsule formulation to 200 mg (four 50 mg CAPsules) taken twice daily.(2) Reduce the dosage of the TABlet formulation to 150 mg (one 150 mg TABlet) twice daily). If the CYP3A4 inhibitor is discontinued, resume the dose of olaparib taken prior to initiation of the CYP3A4 inhibitor after 3 to 5 half-lives.(3) If sonidegib and a moderate CYP3A4 inhibitor must be used, administer the moderate CYP3A4 inhibitor for less than 14 days and monitor closely for adverse effects, particularly musculoskeletal adverse reactions.(4)
DISCUSSION: In an interaction study, itraconazole (a strong CYP3A4 inhibitor) given 200 mg once daily for 14 days followed by a single dose of cobimetinib 10 mg increased mean cobimetinib AUC 6.7-fold (90% CI 5.6, 8.0). Subsequent simulations showed that predicted steady-state concentrations of cobimetinib at a reduced daily dose of 20 mg given with short term use of a moderate CYP3A4 inhibitor were similar to observed steady-state concentrations at the 60 mg dose without an inhibitor.(1) In simulations using physiologically-based pharmacokinetic (PBPK) models, concurrent use of fluconazole, a moderate CYP3A4 inhibitor, may increase the area-under-curve (AUC) of olaparib by 2.2-fold.(2,3) Based upon PBPK simulations, sonidegib mean steady-state AUC would increase 1.8-fold if administered with a moderate CYP3A4 inhibitor for 14 days and would further increase to 2.8-fold if the moderate CYP3A4 inhibitor is coadministered with sonidegib for 4 months.(4) Moderate CYP3A4 inhibitors linked to this monograph include: aprepitant, avacopan, berotralstat, clofazimine, conivaptan, crizotinib, diltiazem, dronedarone, duvelisib, erythromycin, fedratinib, fluconazole, fluvoxamine, fosnetupitant, imatinib, isavuconazonium, ledipasvir, lenacapavir, letermovir, netupitant, nilotinib, schisandra, rilzabrutinib, stiripentol, tofisopam, treosulfan, and verapamil.(5)
There are no moderate interactions for this drug.
Contraindications
The manufacturer states that there are no known contraindications to the use of sonidegib.
- Lactation
- Myalgia
- Myopathy with CK elevation
- Pregnancy
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in 10% or more of patients with advanced basal cell carcinoma receiving sonidegib in the principal efficacy study include muscle spasms, alopecia, dysgeusia, fatigue, nausea, diarrhea, musculoskeletal pain, weight loss, decreased appetite, myalgia, abdominal pain, headache, pain, vomiting, pruritus, and arthralgia.
Laboratory abnormalities reported in more than 15% of patients receiving sonidegib include elevated concentrations of serum creatinine, elevated concentrations of serum CK, hyperglycemia, elevated concentrations of lipase, anemia, lymphopenia, elevated concentrations of aminotransferases (i.e., AST, ALT), and elevated concentrations of amylase.
Amenorrhea lasting at least 18 months also has been reported in 2 of 14 premenopausal women receiving sonidegib (200 or 800 mg once daily).
Rare or Very Rare
- Rhabdomyolysis
More Frequent
- Acute abdominal pain
- Alopecia
- Anemia
- Anorexia
- Diarrhea
- Dysgeusia
- Fatigue
- Headache disorder
- Lymphopenia
- Muscle spasm
- Musculoskeletal pain
- Myalgia
- Nausea
- Pruritus of skin
- Vomiting
- Weight loss
Less Frequent
- General weakness
- Pain
Rare or Very Rare
- Amenorrhea
Precautions
No enhanced messaging available.
Safety and efficacy of sonidegib have not been established in pediatric patients.
Data in animals suggest possible adverse effects on bone, teeth, reproductive tissues, and nerve fibers in juvenile rats receiving sonidegib at exposure levels of approximately 1.2 times the human exposure at the recommended dosage.
Epiphyseal disorders were reported in pediatric patients exposed to sonidegib in a clinical trial.
Sonidegib may cause fetal harm if administered to pregnant females based on its mechanism of action and animal findings.
Verify pregnancy status in all females of reproductive potential prior to initiation of sonidegib therapy. If a female patient or female partner of a male patient receiving sonidegib therapy becomes pregnant during therapy or within 20 or 8 months, respectively, after discontinuance of the drug, the clinician should notify the manufacturer at 800-406-7984.
It is not known whether sonidegib is distributed into milk. Because of the potential for serious adverse reactions to sonidegib in breast-fed infants, women should be advised to discontinue breast-feeding while receiving sonidegib and for at least 20 months after discontinuance of therapy. The effects of the drug on breast-fed infants or on milk production are unknown.
The manufacturer makes no specific dosage recommendations for geriatric patients.
In the BOLT study, 54% of patients receiving sonidegib (200 or 800 mg once daily) were 65 years of age or older and 28% were 75 years of age or older. No overall differences in efficacy were observed between geriatric and younger adults; however, grade 3 or 4 adverse effects, serious adverse effects, or adverse effects requiring interruption or discontinuance of therapy occurred more frequently in patients 65 years of age or older compared with younger adults.
The manufacturer makes no specific dosage recommendations for geriatric patients.
ICD codes
| Code | Type | Description |
|---|---|---|
| Basal cell carcinoma of skin | ||
| C44.01 | ICD10CM | Basal cell carcinoma of skin of lip |
| C44.11 | ICD10CM | Basal cell carcinoma of skin of eyelid, including canthus |
| C44.111 | ICD10CM | Basal cell carcinoma of skin of unspecified eyelid, including canthus |
| C44.112 | ICD10CM | Basal cell carcinoma of skin of right eyelid, including canthus |
| C44.1121 | ICD10CM | Basal cell carcinoma of skin of right upper eyelid, including canthus |
| C44.1122 | ICD10CM | Basal cell carcinoma of skin of right lower eyelid, including canthus |
| C44.119 | ICD10CM | Basal cell carcinoma of skin of left eyelid, including canthus |
| C44.1191 | ICD10CM | Basal cell carcinoma of skin of left upper eyelid, including canthus |
| C44.1192 | ICD10CM | Basal cell carcinoma of skin of left lower eyelid, including canthus |
| C44.21 | ICD10CM | Basal cell carcinoma of skin of ear and external auricular canal |
| C44.211 | ICD10CM | Basal cell carcinoma of skin of unspecified ear and external auricular canal |
| C44.212 | ICD10CM | Basal cell carcinoma of skin of right ear and external auricular canal |
| C44.219 | ICD10CM | Basal cell carcinoma of skin of left ear and external auricular canal |
| C44.31 | ICD10CM | Basal cell carcinoma of skin of other and unspecified parts of face |
| C44.310 | ICD10CM | Basal cell carcinoma of skin of unspecified parts of face |
| C44.311 | ICD10CM | Basal cell carcinoma of skin of nose |
| C44.319 | ICD10CM | Basal cell carcinoma of skin of other parts of face |
| C44.41 | ICD10CM | Basal cell carcinoma of skin of scalp and neck |
| C44.51 | ICD10CM | Basal cell carcinoma of skin of trunk |
| C44.510 | ICD10CM | Basal cell carcinoma of anal skin |
| C44.511 | ICD10CM | Basal cell carcinoma of skin of breast |
| C44.519 | ICD10CM | Basal cell carcinoma of skin of other part of trunk |
| C44.61 | ICD10CM | Basal cell carcinoma of skin of upper limb, including shoulder |
| C44.611 | ICD10CM | Basal cell carcinoma of skin of unspecified upper limb, including shoulder |
| C44.612 | ICD10CM | Basal cell carcinoma of skin of right upper limb, including shoulder |
| C44.619 | ICD10CM | Basal cell carcinoma of skin of left upper limb, including shoulder |
| C44.71 | ICD10CM | Basal cell carcinoma of skin of lower limb, including hip |
| C44.711 | ICD10CM | Basal cell carcinoma of skin of unspecified lower limb, including hip |
| C44.712 | ICD10CM | Basal cell carcinoma of skin of right lower limb, including hip |
| C44.719 | ICD10CM | Basal cell carcinoma of skin of left lower limb, including hip |
| C44.81 | ICD10CM | Basal cell carcinoma of overlapping sites of skin |
| C44.91 | ICD10CM | Basal cell carcinoma of skin, unspecified |
ICD code information from First Databank (FDB).
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Last reviewed · Source: First Databank (FDB) drug data
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