trilaciclib (Rx)

Brand and Other Names:Cosela
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Dosing & Uses

AdultPediatric

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 (total bilirubin ≤ULN and AST >ULN OR total bilirubin 1-1.5x ULN and any AST): No dosage adjustment necessary
  • Moderate-to-severe (total bilirubin >1.5x ULN and any AST): Not studied

Dosing Considerations

Females of reproductive potential: Pregnancy test recommended before initiation

Safety and efficacy not established

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Interactions

Interaction Checker

and trilaciclib

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              Serious - Use Alternative (26)

              • 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.

              • 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)

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                  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)
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                  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

                  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
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                  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.

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                  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])

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                  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
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                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
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                  Formulary

                  FormularyPatient Discounts

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                  The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
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                  ST Step Therapy
                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                  OR Other Restrictions
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                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.