Olaparib
Generic Name: olaparib
Brand Names:
Lynparza
11 DESCRIPTION Olaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor. The chemical name is 4-[(3-{[4-(cyclopropylcarbonyl)piperazin-1-yl]carbonyl}-4-fluorophenyl)methyl]phthalazin-1(2H)-one. The empirical molecular formula for Lynparza is C 24 H 23 FN 4 O 3 and the relative molecular mass is 434.46. It has the following chemical structure: Olaparib is a crystalline solid, is non-chiral and shows pH-independent low solubility across the physiological pH range.
Overview
11 DESCRIPTION Olaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor. The chemical name is 4-[(3-{[4-(cyclopropylcarbonyl)piperazin-1-yl]carbonyl}-4-fluorophenyl)methyl]phthalazin-1(2H)-one. The empirical molecular formula for Lynparza is C 24 H 23 FN 4 O 3 and the relative molecular mass is 434.46. It has the following chemical structure: Olaparib is a crystalline solid, is non-chiral and shows pH-independent low solubility across the physiological pH range.
Uses
1 INDICATIONS AND USAGE Lynparza is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated: Ovarian cancer • for the maintenance treatment of adult patients with deleterious or suspected deleterious germline or somatic BRCA -mutated advanced epithelial ovarian, fallopian tube or primary peritoneal cancer who are in complete or partial response to first-line platinum-based chemotherapy. Select patients for therapy based on an FDA-approved companion diagnostic for Lynparza.
Dosage
2 DOSAGE AND ADMINISTRATION • Recommended dosage is 300 mg taken orally twice daily with or without food. See Full Prescribing Information for the recommended duration. (2.2) • Patients receiving Lynparza for mCRPC should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy. (2.2) • For moderate renal impairment (CLcr 31-50 mL/min), reduce Lynparza dosage to 200 mg orally twice daily. (2.5) 2.1 Patient Selection Information on FDA-approved tests for the detection of genetic mutations is available at http://www.fda.gov/companiondiagnostics .
Side Effects
6 ADVERSE REACTIONS The following adverse reactions are discussed elsewhere in the labeling: • Myelodysplastic Syndrome/Acute Myeloid Leukemia [see Warnings and Precautions (5.1) ] • Pneumonitis [see Warnings and Precautions (5.2) ] • Venous Thromboembolism [see Warnings and Precautions (5.3) ] • Hepatotoxicity, Including Drug-Induced Liver Injury [see Warnings and Precautions (5.4) ] Most common adverse reactions (≥10%): • as a single agent were nausea, fatigue (including asthenia), anemia, vomiting, diarrhea, decreased appetite, headache, dysgeusia, cough, neutropenia, dyspnea, dizziness, dyspepsia, leukopenia, and thrombocytopenia.
Interactions
7 DRUG INTERACTIONS • Strong or moderate CYP3A inhibitors: Avoid concomitant use. If concomitant use cannot be avoided, reduce Lynparza dosage. ( 2.4 , 7.2 , 12.3 ) • Strong or moderate CYP3A inducers: Avoid concomitant use. ( 7.2 , 12.3 ) 7.1 Use with Anticancer Agents Clinical studies of Lynparza with other myelosuppressive anticancer agents, including DNA damaging agents, indicate a potentiation and prolongation of myelosuppressive toxicity. 7.2 Effect of Other Drugs on Lynparza Strong and Moderate CYP3A Inhibitors Coadministration of CYP3A inhibitors can increase olaparib concentrations, which may increase the risk for adverse reactions [see Clinical Pharmacology (12.3) ] . Avoid coadministration of strong or moderate CYP3A inhibitors.
Warnings
5 WARNINGS AND PRECAUTIONS • Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML): Occurred in approximately 1.2% of patients with various BRCA m, g BRCA m, HRR gene-mutated or HRD-positive cancers exposed to Lynparza and the majority of events had a fatal outcome. Monitor patients for hematological toxicity at baseline and monthly thereafter. Discontinue if MDS/AML is confirmed. (5.1) • Pneumonitis: Occurred in 1.0% of patients exposed to Lynparza, and some cases were fatal. Interrupt treatment if pneumonitis is suspected. Discontinue if pneumonitis is confirmed. (5.2) • Venous thromboembolism (VTE), including severe or fatal pulmonary embolism (PE), occurred in patients treated with Lynparza. VTE occurred in 8% of patients with mCRPC. 4 CONTRAINDICATIONS None. None. (4)
Pregnancy
8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action [see Clinical Pharmacology (12.1) ] , Lynparza can cause fetal harm when administered to a pregnant woman. There are no available data on Lynparza use in pregnant women to inform the drug-associated risk. In an animal reproduction study, the administration of olaparib to pregnant rats during the period of organogenesis caused teratogenicity and embryo-fetal toxicity at exposures below those in patients receiving the recommended human dose of 300 mg twice daily (see Data ).
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING Lynparza is available as 150 mg and 100 mg tablets. • 150 mg tablets: green to green/grey, oval, bi-convex, film-coated tablet, with debossment ‘OP150’ on one side and plain on the reverse, are available in: ∘ Bottles of 60 tablets (NDC 0310-0679-60) and ∘ Bottles of 120 tablets (NDC 0310-0679-12).
Frequently Asked Questions
What is Olaparib used for?▼
1 INDICATIONS AND USAGE Lynparza is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated: Ovarian cancer • for the maintenance treatment of adult patients with deleterious or suspected deleterious germline or somatic BRCA -mutated advanced epithelial ovarian, fallopian tube or primary peritoneal cancer who are in complete or partial response to first-line platinum-based chemotherapy. Select patients for therapy based on an FDA-approved companion diagnostic for Lynparza.
What are the side effects of Olaparib?▼
6 ADVERSE REACTIONS The following adverse reactions are discussed elsewhere in the labeling: • Myelodysplastic Syndrome/Acute Myeloid Leukemia [see Warnings and Precautions (5.1) ] • Pneumonitis [see Warnings and Precautions (5.2) ] • Venous Thromboembolism [see Warnings and Precautions (5.3) ] • Hepatotoxicity, Including Drug-Induced Liver Injury [see Warnings and Precautions (5.4) ] Most common adverse reactions (≥10%): • as a single agent were nausea, fatigue (including asthenia), anemia, vomiting, diarrhea, decreased appetite, headache, dysgeusia, cough, neutropenia, dyspnea, dizziness, dyspepsia, leukopenia, and thrombocytopenia.
Can I take Olaparib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action [see Clinical Pharmacology (12.1) ] , Lynparza can cause fetal harm when administered to a pregnant woman. There are no available data on Lynparza use in pregnant women to inform the drug-associated risk. In an animal reproduction study, the administration of olaparib to pregnant rats during the period of organogenesis caused teratogenicity and embryo-fetal toxicity at exposures below those in patients receiving the recommended human dose of 300 mg twice daily (see Data ).
What are the important warnings for Olaparib?▼
5 WARNINGS AND PRECAUTIONS • Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML): Occurred in approximately 1.2% of patients with various BRCA m, g BRCA m, HRR gene-mutated or HRD-positive cancers exposed to Lynparza and the majority of events had a fatal outcome. Monitor patients for hematological toxicity at baseline and monthly thereafter. Discontinue if MDS/AML is confirmed. (5.1) • Pneumonitis: Occurred in 1.0% of patients exposed to Lynparza, and some cases were fatal. Interrupt treatment if pneumonitis is suspected. Discontinue if pneumonitis is confirmed. (5.2) • Venous thromboembolism (VTE), including severe or fatal pulmonary embolism (PE), occurred in patients treated with Lynparza. VTE occurred in 8% of patients with mCRPC. 4 CONTRAINDICATIONS None. None. (4)
Related Medications
Frovatriptan Succinate
frovatriptan succinate
11 DESCRIPTION Frovatriptan succinate tablets contain frovatriptan succinate, a selective 5-hydroxytryptamine1 (5-HT 1B / 1D ) receptor subtype agonist, as the active ingredient. Frovatriptan succinate is chemically designated as R-(+) 3-methylamino-6-carboxamido-1,2,3,4-tetrahydrocarbazole monosuccinate monohydrate and it has the following structure: The molecular formula is C 18 H 23 N 3 O 5 .H 2 O, representing a molecular weight of 379.4 g/mol.
Trifarotene
trifarotene
Retinoid [EPC]
11 DESCRIPTION AKLIEF Cream for topical administration contains 0.005% (50 mcg/g) trifarotene. Trifarotene is a terphenyl acid derivative and is a retinoid. The chemical name of trifarotene is 3”-tert-Butyl-4’-(2-hydroxy-ethoxy)-4”-pyrrolidin-1-yl-[1,1’,3’,1”]terphenyl-4- carboxylic acid.
Terazosin Hydrochloride Dihydrate
terazosin hydrochloride dihydrate
Dosage form: POWDER. Active ingredients: TERAZOSIN HYDROCHLORIDE (25 kg/25kg). Category: BULK INGREDIENT.
Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.