Dosing & Uses
Dosage Forms & Strengths
injection, lyophilized cake for reconstitution
- 300mg (provided as trilaciclib dihydrochloride 349 mg)
Chemotherapy-Induced Myelosuppression
Indicated for adults with extensive-stage small cell lung cancer to reduce chemotherapy-induced myelosuppression when administered before platinum/etoposide-containing or topotecan-containing regimens
240 mg/m2/dose IV completed within 4 hr before chemotherapy on each day chemotherapy is administered
Interval between doses on sequential days should not be >28 hr
Dosage Modifications
Injection-site reactions
- Includes phlebitis and thrombophlebitis
-
Grade 1
- Tenderness with or without symptoms (eg, warmth, erythema, itching)
- Interrupt or slow infusion
- If diluent/flush was 0.9% NaCl, consider changing to D5W for subsequent infusions
-
Grade 2
- Pain, lipodystrophy, edema, phlebitis
- Interrupt infusion
- If pain not severe, follow Grade 1; otherwise, stop infusion in extremity and rotate site of infusion to alternative extremity
- If diluent/flush was 0.9% NaCl, consider changing to D5W for subsequent infusions
- May also consider central access
-
Grade 3 or 4
- Grade 3: Ulceration or necrosis, severe tissue damage; operative intervention indicated OR
- Grade 4: Life-threatening consequences; urgent interventions indicated
- Stop infusion and permanently discontinue
Acute drug hypersensitivity reactions
-
Grade 2
- Moderate; minimal, local, or noninvasive intervention indicated; limiting activities of daily living (ADL)
- Stop infusion and hold until recovery to Grade ≤1 or baseline, then consider resumption
- If Grade 2 recurs, permanently discontinue
-
Grade 3 or 4
- Grade 3: Severe or medically significant, but not immediately life-threatening; hospitalization or prolongation of hospitalization indicated; disabling; limiting self-care ADL OR
- Grade 4: Life-threatening consequences; urgent intervention indicated
- Permanently discontinue
Interstitial lung disease/pneumonitis
-
Grade 2 (symptomatic)
- Hold until recover to Grade ≤1 or baseline
- Consider resumption
-
Permanently discontinue
- Grade 2 recurs
- Grade 3: Severe symptoms; limiting self-care ADL; oxygen indicated
- Grade 4: Life-threatening respiratory compromise; urgent intervention indicated (eg, tracheotomy or intubation)
Other toxicities
-
Hold until recovery to Grade ≤1 or baseline
- Grade 3: Severe/medically significant but not immediately life-threatening; require hospitalization or prolonging hospital stay; disabling; limiting self-care ADL
- Consider resumption
-
Permanently discontinue
- Grade 3 recurs
- Grade 4: Life-threatening consequences, urgent intervention indicated
Renal impairment
- Mild-to-moderate (eGFR 30-89 mL/min/1.73 m2): No dosage adjustment necessary
- Severe (eGFR <30 mL/min/1.73 m2), end-stage renal disease, or dialysis: Not studied
Hepatic impairment
- Mild (Child-Pugh class A): No dosage adjustment necessary
- Moderate or severe (Child-Pugh class B or C): Reduce dose to 170 mg/m2
Dosing Considerations
Females of reproductive potential: Pregnancy test recommended before initiation
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (27)
- amantadine
trilaciclib will increase the level or effect of amantadine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- amiloride
trilaciclib will increase the level or effect of amiloride by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- cimetidine
trilaciclib will decrease the level or effect of cimetidine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- ciprofloxacin
trilaciclib will decrease the level or effect of ciprofloxacin by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- cisplatin
trilaciclib will increase the level or effect of cisplatin by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with cisplatin. Risk of increased cisplatin kidney exposure and altered net accumulation, which may associate with dose-related nephrotoxicity. Closely monitor for nephrotoxicity.
- dalfampridine
trilaciclib will increase the level or effect of dalfampridine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with dalfampridine. Consider potential benefits of trilaciclib against risk of seizures with increased dalfampridine blood levels.
- dofetilide
trilaciclib will decrease the level or effect of dofetilide by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with dofetilide. Consider potential benefits of trilaciclib against risk of QT interval prolongation with increased dofetilide blood levels.
- dopamine
trilaciclib will decrease the level or effect of dopamine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- etrasimod
etrasimod, trilaciclib. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Risk of additive immune system effects with etrasimod has not been studied in combination with antineoplastic, immune-modulating, or noncorticosteroid immunosuppressive therapies. Avoid coadministration during and in the weeks following administration of etrasimod. .
- famotidine
trilaciclib will decrease the level or effect of famotidine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- ganciclovir
trilaciclib will decrease the level or effect of ganciclovir by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- guanidine
trilaciclib will decrease the level or effect of guanidine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- lamivudine
trilaciclib will decrease the level or effect of lamivudine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- levofloxacin
trilaciclib will decrease the level or effect of levofloxacin by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- memantine
trilaciclib will decrease the level or effect of memantine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- metformin
trilaciclib will decrease the level or effect of metformin by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- nadolol
trilaciclib will decrease the level or effect of nadolol by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- oxaliplatin
trilaciclib will decrease the level or effect of oxaliplatin by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- pindolol
trilaciclib will decrease the level or effect of pindolol by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- pramipexole
trilaciclib will decrease the level or effect of pramipexole by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- procainamide
trilaciclib will decrease the level or effect of procainamide by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- ranitidine
trilaciclib will decrease the level or effect of ranitidine by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- relebactam
trilaciclib will decrease the level or effect of relebactam by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- topotecan
trilaciclib will decrease the level or effect of topotecan by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- trifluridine/tipiracil
trilaciclib will decrease the level or effect of trifluridine/tipiracil by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- trimethoprim
trilaciclib will decrease the level or effect of trimethoprim by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
- varenicline
trilaciclib will decrease the level or effect of varenicline by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of trilaciclib (OCT2, MATE1, and MATE-2K inhibitor) with substrates where minimal increased concentration in kidney or blood may lead to serious or life-threatening toxicities.
Monitor Closely (0)
Minor (0)
Adverse Effects
>10%
All grades
- Fatigue (34%)
- Hypocalcemia (24%)
- Hypokalemia (22%)
- Hypophosphatemia (21%)
- AST increased (17%)
- Headache (13%)
Grade ≥3
- Neutropenia (32%); placebo (69%)
- Thrombocytopenia (18%); placebo (33%)
- Anemia (16%); placebo (34%)
1-10%
All grades
Pneumonia (10%)
- Rash (9%)
- Infusion-related reaction (8%)
- Peripheral edema (7%)
- Upper abdominal pain (7%)
- Thrombosis (7%)
- Hyperglycemia (6%)
- Grade ≥3 H4
- Hypophosphatemia (7%)
- Pneumonia (7%)
- Hypokalemia (6%)
- Leukopenia (4%); placebo (17%)
- Fatigue (3%)
- Thrombosis (3%)
- Febrile neutropenia (3%); placebo (9%)
- Hemorrhage (>3%)
- Respiratory failure (≥2%)
- Hyperglycemia (2%)
- Asthenia (2%)
<1%
Grade ≥3
- Cerebrovascular accident
- Ischemic stroke
- Hemoptysis
- Myositis
- Lymphopenia
- Acute respiratory failure (fatal)
Warnings
Contraindications
History of serious hypersensitivity to trilaciclib
Cautions
Severe, life-threatening, or fatal interstitial lung disease (ILD) and/or pneumonitis reported with cyclin-dependent kinases (CDK)4/6 inhibitors, including trilaciclib; monitor for symptoms (eg, cough, dyspnea, hypoxia)
May cause fetal harm
This drug is mainly metabolized in the liver; drug exposure is increased with moderate and severe hepatic impairment (Child-Pugh classes B and C)
Injection-site reactions
- Injection-site reactions (eg, phlebitis, thrombophlebitis) may occur
- Median time to onset: 15 days (from initiation); 1 day (preceding dose)
- Median duration: 1 day
- Monitor for signs and symptoms, including infusion-site pain and erythema during infusion
Acute drug hypersensitivity reactions
- May cause acute drug hypersensitivity reactions, including facial edema and urticaria
- Median time to onset: 77 days (from initiation); 1 day (preceding dose)
- Median duration: 6 day
- Monitor for signs and symptoms, including facial, eye, and tongue edema, urticaria, pruritus, and anaphylactic reactions
Drug interaction overview
- Inhibitor of OCT2, MATE1, MATE-2K
-
Certain OCT2, MATE1, and MATE-2K substrates
- Avoid coadministration
- Trilaciclib may increase plasma and/or kidney concentrations of certain OCT2, MATE1, and MATE-2K substrates (eg, dofetilide, dalfampridine, cisplatin)
- Even minimal changes in concentrations may lead to serious or life-changing toxicities
Pregnancy & Lactation
Pregnancy
Based on mechanism of action, fetal harm may occur when administer to pregnant females
No human or animal data are available
Advise pregnant females of potential risks to fetus
Pregnancy test recommended in females of reproductive potential
Contraception
- Females of reproductive potential: Use effective contraception during treatment and for at least 3 weeks after final dose
Infertility
- No studies performed
- Based on animal studies, fertility may be impaired in females of reproductive potential
Lactation
No data are available
Advise to not breastfeed during treatment and for at least 3 weeks after last dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Transient CDK 4/6 inhibitor
Hematopoietic stem and progenitor cells (HSPC) in the bone marrow give rise to circulating neutrophils, red blood cells, and platelets
HSPC proliferation is dependent on CDK4/6 activity
Distribution
Blood-to-plasma ratio:1.21-1.53
Vd: 1,130 L
Metabolism
Extensively metabolized
Trilaciclib is the predominantly circulating compound in plasma following IV administration, representing ~50% of plasma total radioactivity
Elimination
Half-life: ~14 hr
Estimated clearance: 158 L/hr
Excretion: Feces (79.1% [7% unchanged]); urine (14% [2% unchanged])
Administration
IV Compatibilities
D5W
0.9% NaCl
IV Preparation
Reconstitution
- Calculate dose, total drug volume, and number of vials needed
- Reconstitute each 300-mg vial with 19.5 mL of 0.9% NaCl or D5W, obtaining a concentration of 15 mg/mL
- Gently swirl vial for up to 3 min until sterile lyophilized cake completely dissolves; do not shake
- Visually inspect for discoloration and particulate matter; reconstituted solution should be a clear, yellow solution; discard if discolored, cloudy, or contains visible particulates
Dilution
- Withdraw required dosage volume from reconstituted vial(s); dilute into 0.9% NaCl or D5W IV infusion bag to obtain final concentration of 0.5-3 mg/mL
- Gently invert diluted solution to mix; do not shake
- Visually inspect for particulate matter and discoloration; diluted solution is a clear, yellow solution
IV Administration
Infuse over 30 min
Complete infusion within 4 hr before starting chemotherapy
Administer with an infusion set, including an in-line 0.2- or 0.22-micron filter; compatible in-line filters include polyethylene sulfone, polyvinylidene fluoride, and cellulose acetate
Flush infusion line/cannula with sterile 0.9% NaCl or D5W once infusion completes
Do NOT administer or coadminister with
- Polytetrafluorethylene (PTFE) in-line filters: Diluted solutions are incompatible with PTFE in-line filters
- Other drugs through same infusion line
- Other drugs through a central access device unless device supports coadministration of incompatible drug(s)
Missed dose
- Discontinue chemotherapy on day dose was missed
- Consider resuming both trilaciclib and chemotherapy on next scheduled chemotherapy
Discontinuing treatment
- Wait 96 hr from last trilaciclib dose before resumption of chemotherapy only
Storage
Unopened vial
- Store at 20-25ºC (68-77ºF); excursion permitted to 15-30ºC (59-86ºF)
Reconstituted vial
- Store at 20-25ºC (68-77ºF) for up to 4 hr before transfer to infusion bag; do not refrigerate or freeze; discard any unused portion after use
- Do not refrigerate or freeze
Diluted solution
-
D5W
- IV infusion bag material (polyvinyl chloride [PVC], ethylene vinyl acetate [EVA], polyolefin [PO], or polyolefin/polyamide [PO/PA])
- Store at 20-25ºC (68-77ºF) for up to 12 hr
-
0.9% NaCl
- IV infusion bag material (PVC, EVA, or PO): Store at 20-25ºC (68-77ºF) for up to 8 hr
- IV infusion bag material (PO/PA): Store at 20-25ºC (68-77ºF) for up to 4 hr
Images
Formulary
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